AZD7545_252017-04-2_DataSheet_MedChemExpress

Product Name:

AZD7545CAS No.:

252017-04-2Cat. No.:

HY-16082

Product Data Sheet

MWt:

478.87Formula:

C19H18ClF3N2O5S Purity :>98%

Solubility:

DMSO

Mechanisms:

Biological Activity:

AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of

Pathways:Others; Target:PDHK ,()

36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.

IC50 Value: 36.8 nM (PDHK1); 6.4 nM (PDHK2) [1]

Target: PDHK1/2in vitro: The IC50 values for inhibition of PDHK2 and PDHK1 by AZD7545 were 6.4 ± 2.2 nM (n = 6)and 36.8 ± 18 nM (n = 3) respectively. Other compounds in this series inhibited both PDHK1 and PDHK2 and a consistent trend of reduced potency (5-15-fold) towards PDHK1, as compared with PDHK2, was observed. In contrast, AZD7545 and related compounds failed to inhibit PDHK4 and paradoxically, at higher concentrations (>10 nM), AZD7545 stimulated PDHK4 activity [1]. In the f PDHK2AZD7545i d PDH ti it ith EC(50)l f 52M I t References:

[1]. Morrell JA, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem

Soc Trans. 2003 Dec;31(Pt 6):1168-70.[2]Mayers RM et al AZD7545a novel inhibitor of pyruvate dehydrogenase kinase 2(PDHK2)presence of PDHK2, AZD7545 increased PDH activity with an EC(50) value of 5.2 nM. In rat

hepatocytes, the rate of pyruvate oxidation was stimulated 2-fold (EC(50) 105 nM) [2].in vivo: A single d...

[2]. Mayers RM, et al. AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2),activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa)

Zucker rats. Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7.Caution: Not fully tested. For research purposes only

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