AZD7545

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD7545 是一种有效的 PDHK 抑制剂。

AZD7545 is an inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) (IC50 value of 6.4nM ) for the treatment of type 2 diabetes. AZD7545 activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats.

AZD7545 (10 μM; 90 hours for BRAFV600E human melanoma cells and 120 hours for NRAS mut human melanoma cells) specifically suppresses growth of cells harboring BRAF and NRAS mutations as well as in inhibitor-resistant human melanoma. Cell Proliferation Assay Cell Line:Human melanoma cells lines of BRAFV600E (A375, IGR37) and NRASmut (SKMel30, IPC298, MelJuso)Concentration:10 μM Incubation Time:90 hours (BRAFV600E human melanoma cells) and 120 hours (NRAS mut human melanoma cells) Result:Mediated growth suppression of BRAFV600E mutant and NRAS mut human melanoma cells.

A single dose of AZD7545 (Oral administration; 10 mg/kg once a day (08:00 h) or Twice a day (08:00 and 18:00 h); for 7 days) to Wistar rats increases the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner. A single dose of 10 mg/kg also significantly elevates muscle PDH activity in obese Zucker (fa/fa) rats. Animal Model:Obese male (fa/fa) Zucker rats Dosage:10 mg/kg Administration:Oral administration; once a day (08:00 h) or Twice a day ( 08:00 and 18:00 h); for 7 days Result:Improved the control of blood glucose levels.

AZD7545 | AZD-7545 | AZD 7545

Immunology/Inflammation

Hydroxylase

PDHK1| PDHK2

Metabolic Disease

——

252017-04-2

478.87

C19H18ClF3N2O5S

>98% (HPLC)

DMSO : ≥ 46 mg/mL; 96.06 mM

O=C(N(C)C)c1ccc(S(=O)(=O)c2ccc(NC(=O)[C@@](C)(O)C(F)(F)F)c(Cl)c2)cc1

4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide

(-20℃)

With Ice Pack

≥ 2 years