Curdione_DataSheet_MedChemExpress
Resiquimod_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Resiquimod is a Toll–like receptor 7 and 8 (TLR7/TLR8) agonist that induces the levels of cytokines such as TNF–α, IL–6 and IFN–α.In Vitro: Resiquimod (R–848) induces both hapten– and allergen–specific circulating T cells, including TH2 effectors, to produce IFN–γ and even to lose the ability to produce IL–4[2]. Resiquimod (R848) enhances PBL proliferation in a dose–dependent manner,and increases the number of BrdU–positive cells in BrdU incorporation assay. Cells treated with R848 exhibits significantly increased (3.5–fold) luciferase (a reporter of NF–κB activity) activity [3].In Vivo: Resiquimod (R–848) (50 μg/bird, i.m. route) significantly up–regulates the expression of IFN–α, IFN–β, IFN–γ, IL–1β, IL–4,iNOS and MHC–II genes in SPF chicken [1].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[3]For luciferase assay, FG–9307 cells are transfected with the firefly NF–κB–specific luciferase reporter vector pNFκB–Met–Luc2. Transfection efficiency is monitored by co–transfection with the pSEAP2 control vector, which constitutivelyexpresses the human secreted enhanced alkaline phosphatase (SEAP). Then the cells are treated with Resiquimod (R848, 1 μg/mL), CQ (10 μM), CQ plus R848 or PBS and incubated at 22°C for 24 h. The culture medium of the transfectants is then analyzed for luciferase activity and SEAP activity using Luciferase Assay Kit and the Great EscAPe? SEAP Chemiluminescence Detection Kit, respectively. The assay is performed three times.Cell Assay: Resiquimod is dissolved in DMSO.[3]For inhibition of lysosomal acidification, cells are incubated with 10 μM CQ for 1 h before Resiquimod (R848) treatment. After treatment, 20 μL of 5 mg/mL MTT is added to the plate. The plate is incubated at 22°C for 4 h, and 200 μL dimethyl sulfoxide is added to the plate to dissolve the reduced formazan. The plate is then read at 490 nm with a microplate reader. To determine the effect of Myd88 inhibition on R848–induced cell proliferation, the Myd88 inhibitor Pepinh–MYD and the control peptide Pepinh–Control are added to PBL at the concentration of 50 μM, and the plate is incubated at 22°C for 6 h.After incubation, the cells are treated with R848 and subjected to MTT assay as above. To determine the effect of NF–κB inactivation on R848–induced cell proliferation, BAY–11–7082, an irreversible inhibitor of IκB–α phosphorylation, is added to the cells at the concentration of 1 μM, and the plate is incubated at 22°C for 1 h. After incubation, the cells are treated with R848 and subjected to MTT assay as earlier. All experiments are performed three times.Animal Administration: Resiquimod is dissolved in PBS.[1]A total of 40 SPF chickens of two–week old are allotted to one of the following four experimental groups (n=10/group): Group A: PBS control; Group B: inactivated NDV vaccine; Group C:commercial oil adjuvanted inactivated NDV vaccine prepared from lentogenic strain and Group D: combination of inactivated NDV vaccine and R–848 (50 μg/bird). Vaccine or PBS is administered by intramuscular route in the thigh muscle. A booster dose is given 14–day post immunization (d.p.i). Two weeks post–booster, experimental SPF birds are challenged with velogenic strain of NDV (105 ELD 50 per bird) intramuscularly. Clinical signs and mortality are observed daily till 14 day post–challenge (d.p.c).Cloacal swabs (n=6/group) are collected from the birds on day 0, 4, 7 and 14 post–challenge and inoculated into 10–day oldProduct Name:Resiquimod Cat. No.:HY-13740CAS No.:144875-48-9Molecular Formula:C 17H 22N 4O 2Molecular Weight:314.38Target:Toll–like Receptor (TLR)Pathway:Immunology/Inflammation Solubility:DMSO: ≥ 30 mg/mLembryonated chicken eggs (n=3 eggs/sample) through intra–allantoic route. Three day post–inoculation, the allantoic fluid is checked for the NDV growth by spot haemagglutination using 10% chicken RBC.References:[1]. Sachan S, et al. Adjuvant potential of resiquimod with inactivated Newcastle disease vaccine and its mechanism of action in chicken. Vaccine. 2015 Aug 26;33(36):4526–32.[2]. Brugnolo F, et al. The novel synthetic immune response modifier R–848 (Resiquimod) shifts human allergen–specific CD4+ TH2 lymphocytes intoIFN–gamma–producing cells. J Allergy Clin Immunol. 2003 Feb;111(2):380–8.[3]. Zhou ZX, et al. Immune effects of R848: evidences that suggest an essential role of TLR7/8–induced, Myd88– and NF–κB–dependent signaling in the antiviral immunity of Japanese flounder (Paralichthys olivaceus). Dev Comp Immunol. 2015 Mar;49(1):113–20.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
Solifenacin_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Solifenacin is a novel muscarinic receptor antagonist with pK i s of 7.6, 6.9 and 8.0 for M 1, M 2 and M 3 receptors, respectively.IC50 & Target: pKi: 7.6 (M 1 receptor), 6.9 (M 2 receptor), 8.0 (M 3 receptor)[1]In Vitro: Solifenacin is a novel muscarinic receptor antagonist with pK i s of 7.6±0.056, 6.9±0.034 and 8.0±0.021 for M1, M2 and M3receptors, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin and oxybutynin on Ca 2+ m obilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin does not shift the CCh dose–activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pK b values are obtained as 7.4±0.17 for Solifenacin and8.8±0.21 for oxybutynin [1].In Vivo: Solifenacin reduces bladder responses by 40% at a dose of 210 nmol/kg (0.1 mg/kg) and abolishes them at 2100 nmol/kg (1mg/kg). In contrast, its inhibitory effects on salivary and cardiac responses are only slight at 630 nmol/kg (0.3 mg/kg), and reach 66%and 49%, respectively, at 2100 nmol/kg (1 mg/kg). At doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), Solifenacin slightly increases saliva secretion [1]. Solifenacin (0.01 to 0.3 mg/kg i.v.) dose–dependently increases bladder capacity and voided volume atdoses of 0.03 mg/kg i.v. or more, but does not affect residual volume or micturition pressure at any dose tested [2].PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[1]Cytosolic Ca 2+ mobilization is determined in guinea pig detrusor cells. Briefly, single detrusor cells are prepared from epithelium–free bladders, loaded with Fura 2, and suspended in phenol red–free Hanks’ balanced salt solution supplemented with 20mM HEPES (pH=7.4) and 0.1% bovine serum albumin (HBSS–H/B). A 490 μL aliquot of the cell suspension is continuously stirred, kept at 28°C and monitored for the ratio of fluorescence at 500 nm with excitation at 340 nm to that at 380 nm. To each aliquot, 5 μL of test drug (including Solifenacin) and stimulant solutions are serially added with a 2 min interval, and the peak increase over the level just before stimulation is used for data analysis [1].Animal Administration:[2]Male rats (270 to 320 g) are used in this study. After the measurement of neurological deficits, cystometry is performed. Briefly, conscious rats showing a moderate to severe neurological deficit (score: 4 to13) are placed in a restraining cage. To facilitate drug (including Solifenacin) evaluation, only those animals showing urinary frequency are eligible for study. The bladder is emptied by drainage of urine through the catheter and then continuously re–infused with saline. After stable voiding cycles are established, each rat receives a single intravenous administration of test drug (including Solifenacin) at a volume of 1 ml/kg [2]. References:[1]. Ikeda K, et al. M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland. Naunyn SchmiedebergsProduct Name:Solifenacin Cat. No.:HY-A0034CAS No.:242478-37-1Molecular Formula:C23H26N2O2Molecular Weight:362.46Target:mAChR Pathway:GPCR/G Protein; Neuronal Signaling Solubility:10 mM in DMSOArch Pharmacol. 2002 Aug;366(2):97–103.[2]. Suzuki M, et al. Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarctedrats. Eur J Pharmacol. 2005 Apr 4; 512(1):61–6.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
A939572_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC 50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.IC50 & Target: IC50: <4 nM (mSCD1), 37 nM (hSCD1)[1]In Vitro: A939572 exhibits robust in vivo activity with dose–dependent desaturation index lowering effects [1]. A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose–dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC 50s of 65 nM, 50 nM, 65 nM, and 6 nM, respectively). In A939572 (SCDi)treated Caki1 and A498 cells, all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control, and this elevated expression can be blocked with the addition of OA–BSA [2].In Vivo: Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg, p.o.) and Tem individually or in combination over the course of four weeks, and tumor volume (mm 3) is recorded. A939572 and Tem monotherapy generate similar growth responses with approximately 20–30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment. The combination group yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1week of treatment [2].PROTOCOL (Extracted from published papers and Only for reference)Cell Assay: A939572 is dissolved in DMSO and stored, and then diluted with appropriate media before use [2].[2]Cells are plated (0.5 or 1×105/well) in 24–well plates in triplicate. Cells are counted using a Coulter Particle Counter. Oleic acid–albumin isadded to media at 5μMol. A939572 stocks are prepared in DMSO. Temsirolimus dosing is performed. Soft agar cultures are prepared by diluting 2× growth medium 1:1 in 1.5% Seaplaque ®GTG ® agarose, with 500 cells/plate in 60mm culture dishes.Colonies are stained with Giemsa and counted after 3wks [2].Animal Administration: A939572 is re–suspended in strawberry flavored Kool–Aid ® in sterilized H 2O (Mice)[2].[2]Mice [2]A498 cells are subcutaneously implanted in athymic nu/nu mice at 1×106 cells/mouse in 50% Matrigel. Tumors reach ~50 mm 3 prior to 4 wk treatment. A939572 is re–suspended in strawberry flavored Kool–Aid ® in sterilized H 2O (0.2 g/mL) vehicle at 30 mg/kg in a 50μL dose. Mice are orally fed by using a syringe to administer the 50 μL dose twice daily/mouse. This modified method is found to be effective and less stressful on the mice. Temsirolimus is solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10 mg/kg in a 50 μL dose once every 72 hrs/mouse. Tumor volumes are calculated using the formula 0.5236 (L*W*H) and body weight are measured every 3 days.References:[1]. Xin Z, et al. Discovery of piperidine–aryl urea–based stearoyl–CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298–302.Product Name:A939572Cat. No.:HY-50709CAS No.:1032229-33-6Molecular Formula:C 20H 22ClN 3O 3Molecular Weight:387.86Target:Stearoyl–CoA Desaturase (SCD)Pathway:Metabolic Enzyme/Protease Solubility:DMSO: ≥ 56 mg/mL[2]. von Roemeling CA, et al. Stearoyl–CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368–80.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
EG00229_SDS_MedChemExpress
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:May-24-2017Print Date:May-24-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :EG00229Catalog No. :HY-10799CAS No. :1210945-69-91.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:EG 00229; EG⁻00229Formula:C19H20F3N7O7S3Molecular Weight:611.60CAS No. :1210945-69-94. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance Light yellow to yellow (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
MK-2894-SDS-MedChemExpress
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Oct.-12-2018Print Date:Oct.-12-20181. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :MK-2894Catalog No. :HY-10413CAS No. :1006036-87-81.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:NoneFormula:C25H22F3NO3SMolecular Weight:473.51CAS No. :1006036-87-84. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2018 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
Febuxostat_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.IC50 value: 0.6 nM (Ki) [1]Target: xanthine oxidasein vitro: Febuxostat displays potent mixed–type inhibition of the activity of purified bovine milk xanthine oxidase, with Ki and Ki' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase [1].in vivo: Febuxostat (5–6 mg/kg/day) combined with fructose significantly lowers blood pressure, UA, triglycerides, and insulin in rats compared with fructose alone. Febuxostat (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone [2]. Febuxostat prevents hyperuricemia in 5/6nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) rats and ameliorates proteinuria, preserves renal function and prevents glomerular hypertension in both 5/6 nephrectomy (5/6 Nx)+vehicle (V)+Febuxostat(Fx) and 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) groups [3]. Febuxostat (5 mg/kg/d by gavage for 8 days) treatment after transverse aortic constriction (TAC)attenuates the TAC–induced left ventricular (LV) hypertrophy and dysfunction. Febuxostat blunts the TAC–induced increases innitrotyrosine (indicating reduced myocardial oxidative stress), p–Erk(Thr202/Tyr204), and p–mTOR(Ser2488), with no effect on total Erk or total mTOR [4].References:[1]. Takano Y, et al. Selectivity of febuxostat, a novel non–purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci, 2005, 76(16), 1835–1847.[2]. Sánchez–Lozada LG, et al. Effects of febuxostat on metabolic and renal alterations in rats with fructose–induced metabolic syndrome. Am J Physiol Renal Physiol, 2008, 294(4), F710–F718.[3]. Sánchez–Lozada LG, et al. Effect of febuxostat on the progression of renal disease in 5/6 nephrectomy rats with and without hyperuricemia. Nephron Physiol, 2008, 108(4), p69–p78.[4]. Xu X, et al. Xanthine oxidase inhibition with febuxostat attenuates systolic overload–induced left ventricular hypertrophy and dysfunction in mice. Card Fail, 2008, 14(9), 746–753.Product Name:Febuxostat Cat. No.:HY-14268CAS No.:144060-53-7Molecular Formula:C 16H 16N 2O 3S Molecular Weight:316.37Target:Xanthine Oxidase Pathway:Metabolic Enzyme/Protease Solubility:10 mM in DMSOCaution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
AZD3514_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.IC50 Value: 2.2 uM (Ki)Target: androgen receptorAZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors [1].in vitro: AZD3514 inhibits cell growth in prostate cancer cells expressing wild–type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR–negative prostate cancer cells, indicating a dependency on AR for efficacy [2].in vivo: We assessed activity initially in the Hershberger castrated rat assay in which oral dosing of AZD3514 (100mg/kg once–daily for 7 days) significantly inhibited testosterone–induced growth of sexual accessory organs [2].Clinical trial: Open–label Prostate Cancer Study. Phase 1References:[1]. Bradbury RH, et al. Discovery of AZD3514, a small–molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1945–8.[2]. Sarah A Loddick, Rob Bradbury, Nicola Broadbent. Abstract 3848: Preclinical profile of AZD3514: A small molecule–targeting androgen receptor function with a novel mechanism of action and the potential to treat castration–resistant prostate cancer. Cancer Research: April 15, 2012; Volume 72, Issue 8,Supplement 1Product Name:AZD3514Cat. No.:HY-16079CAS No.:1240299-33-5Molecular Formula:C 25H 32F 3N 7O 2Molecular Weight:519.56Target:Androgen Receptor Pathway:Others Solubility:10 mM in DMSOCaution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
Cediranib_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Cediranib is a highly potent VEGFR(KDR) inhibitor with IC 50 of <1 nM, and also inhibits Flt1/4 with IC 50 of 5 nM/≤3 nM, with similar activity against c–Kit and PDGFRβ, 36–, 110–fold and is >1000–fold selective more for VEGFR than PDGFR–α, CSF–1R and Flt3.IC50 & Target: IC50: 0.5 nM (VEGFR2), 5 nM (Flt1), ≤ 3 nM (Flt4)In Vitro: Cediranib inhibits VEGF–stimulated proliferation with IC 50 of 0.4 nM. Cediranib suppresses PDGF–AA with IC 50 of 0.04 μM in MG63 cell lines. Cediranib has been shown to block Flt1–associated kinase with IC 50 of 5 nM and VEGF–C and VEGF–D receptor Flt–4with IC 50 less than 3 nM. In addition, the IC 50 values for inhibition of c–Kit and PDGFRβ tyrosine kinase are 2 nM and 5 nMrespectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro [1].In Vivo: Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF–induced angiogenesis.Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated [1]. Single agent cediranib or SC68896 treatment does not alter tumor growth or survival, combined cediranib/SC68896significantly delays malignant glioma and increases median survival in mice [2]. PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[1]Cediranib is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective K m for ATP (0.2–30 μM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt–1, Flt–4, c–Kit, PDGFRα, PDGFRβ, CSF–1R, Flt–3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR),ErbB2, Aurora A, and Aurora B] using ELISA. Selectivity versus CDK2 and CDK4 serine/threonine kinases is examined usingscintillation proximity assays with a retinoblastoma substrate and [γ–33P]ATP. Activity of Cediranib is compared to MAPKkinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [γ–33P]ATP, and paper capture/scintillationcounting.Cell Assay: AZD2171 Is prepared initially as a 10 mM stock solution in DMSO.[1]The proliferation of the HUVEC cell line is evaluated in the presence and absence of growth factors by measuring 3H–thymidine incorporation following a 4–day incubation period.Proliferation of MG63 osteosarcoma cells is induced by PDGF–AA, which selectively activates signaling of the PDGFRα homodimer.HUVEC and MG63 osteosarcoma cells are cultured in DMEM without phenol red containing 1% charcoal stripped FCS, 2 mMglutamine, and 1% nonessential amino acids for 24 hours. Cediranib or vehicle is added with PDGF–AA ligand (50 ng/mL) and plates incubated for another 72 hours. Cellular proliferation is determined using bromodeoxyuridine ELISA.Animal Administration: AZD2171 is suspended in 1% (w/v) aqueous polysorbate 80 (polyoxyethylene, sorbitan mono–oleate in deionized water) for mice study. AZD2171 is suspended in a 0.5% (w/v) hydroxypropyl methylcellulose solution containing 0.1%(w/v) aqueous polysorbate 80 for rat study. [1] Mice [1]Product Name:Cediranib Cat. No.:HY-10205CAS No.:288383-20-0Molecular Formula:C 25H 27FN 4O 3Molecular Weight:450.51Target:VEGFR; Autophagy Pathway:Protein Tyrosine Kinase/RTK; Autophagy Solubility:DMSO: ≥ 49 mg/mLProtocols for establishing s.c. PC–3, Calu–6, SKOV–3, MDA–MB–231, and SW620 tumors in female nude (nu/nu genotype) mice are as described previously (29, 30). When tumors reached a volume of 0.1 to 0.5 cm3, mice are randomized (6–12 per group) and AZD2171 (0.75–6 mg per kg per day) or vehicle given once daily by oral gavage. Tumor volumes are assessed by bilateral Vernier caliper measurement at least twice weekly and calculated. Growth inhibition is calculated from the start of treatment by comparison of the mean change in tumor volume for control and treated groups. To remove any size dependency before statistical evaluation (the variance in mean tumor volume data increases proportionally with volume and is therefore disproportionate between groups), data is log–transformed before statistical evaluation using a one–tailed two–sample t test.Rat[1]Young female Alderley Park rats (6 weeks of age, n=5) are dosed orally, once daily for 28 days with AZD2171 (1.25–5 mg per kg per day) or vehicle. Additional rats (five per group) are treated with AZD2171 (5 mg per kg per day) or vehicle for 28 days and maintained for a further 28 days without treatment, to examine the effect of compound withdrawal. Histologic paraffin wax sections of the femorotibial joints and ovaries are stained with H&E. Morphometric image analysis of femorotibial sections is done, with growth plate areas from both the femur and tibia in each joint being combined for an analysis of the effect of compound treatment. The area of corpora lutea in H&E–stained ovary sections is similarly determined by morphometric analysis.References:[1]. Wedge SR, et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor–2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res, 2005, 65(10), 4389–4400.[2]. Lobo MR, et al. Synergistic Antivascular and Antitumor Efficacy with Combined Cediranib and SC6889 in Intracranial Mouse Glioma. PLoS One. 2015 Dec 8;10(12):e0144488.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
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Inhibitors, Agonists, Screening Libraries
Data Sheet
BIOLOGICAL ACTIVITY:
Curdione, one of the major sesquiterpene compounds from Rhizoma Curcumae, has been shown to exhibit multiple bioactive properties.
IC50 value: 60–80 μM
Target:
In vitro: The study of the influence of curdione on the hemorheological changes in blood stasis model rats and thrombolysis in vitro showed that curdione only possessed thrombolytic effect in dose of 0.235 g.L–1 and 2.35 g.L–1, but has not the notable activity of thrombolysis [1]. The effects of curdione on human platelet aggregation induced by thrombin (0.3 U/ml) were tested in vitro. Curdione preferentially inhibited PAF– and thrombin– induced platelet aggregation in a concentration–dependent manner (IC50: 60–80 μM),whereas much higher concentrations of curdione were required to inhibit platelet aggregation induced by ADP and AA. Curdione also inhibited P–selectin expression in PAF–activated platelets. Moreover, curdione caused an increase in cAMP levels and attenuated intracellular Ca2+ mobilization in PAF–activated platelets.
In vivo: Curdione showed significant antithrombotic activity [2].
References:
[1]. SI Li, et al. Effect of curdione on hemorheological indexs in rats with blood stasis syndrome. Anhui Medical and Pharmaceutical Journal, 2012–09
[2]. Quan Xia, et al. Inhibition of platelet aggregation by curdione from Curcuma wenyujin essential Oil. Thrombosis Research Volume 130, Issue 3,September 2012, Pages 409–414
Product Name:
Curdione Cat. No.:
HY-N0353CAS No.:
13657-68-6Molecular Formula:
C 15H 24O 2Molecular Weight:
236.35Target:
Others Pathway:
Others Solubility:
10 mM in DMSO
Caution: Product has not been fully validated for medical applications. For research use only.
Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。