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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Pyruvate Dehydrogenase Kinase (PDK)-AZD7545
AZD7545

Chemical Structure : AZD7545

CAS No.: 252017-04-2

AZD7545 (AZD-7545)

货号: PC-23744Not For Human Use, Lab Use Only.

AZD7545 is a potent, selective inhibitor of pyruvate dehydrogenase kinase (PDHK, PDK) with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD7545 is a potent, selective inhibitor of pyruvate dehydrogenase kinase (PDHK, PDK) with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.
AZD7545 increases PDH activity with EC50 of 5.2 nM, stimulates the rate of pyruvate oxidation 2-fold (EC50=105 nM) in rat hepatocytes.
AZD7545 inhibits PDHK activity of recombinant PDHK and intracellular PDH phosphorylation.

物理化学性质&存储条件

分子量 478.87
分子式 C19H18ClF3N2O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-4-((3-Chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenyl)sulfonyl)-N,N-dimethylbenzamide

参考文献

1. Mayers RM, et al. Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7.

2. Morrell JA, et al. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70.

3. Makita N, et al. J Pharm Pharmacol. 2017 Jan;69(1):43-51.

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