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AZD7545
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD7545图片
CAS NO:252017-04-2
规格:98%
分子量:478.87
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
PDHK inhibitor,potent and selective
CAS:252017-04-2
分子式:C19H18ClF3N2O5S
分子量:478.87
纯度:98%
存储:Store at -20°C

Background:

AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) with IC50 value of 6.4nM [1].


PDH catalyzes the decarboxylation of pyruvate, converting it to acetyl-CoA. This enzyme is regulated by PDH kinases. The inhibitor of PDHK is developed for the treatment of type 2 diabetes. AZD7545 is a selective inhibitor of PDHK2. It inhibits PDHK1 and PDHK2 with IC50 values of 36.8nM and 6.4nM, respectively. Besides that, AZD7545 increases PDH activity with EC50 value of 5.2nM when using recombinant human PDHK2. In vivo studies show that administration of AZD7545 significantly activates PDH activity in liver and partially activates PDH activity in skeletal muscle and heart. In Zucker (fa/fa) rats, AZD7545 at dose of 10 mg/kg increases muscle PDH from 61% to 97% active and liver PDH from 33.5% to 72.8% [1, 2].


参考文献:
[1] Morrell J A, Orme J, Butlin R J, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochemical society transactions, 2003, 31(6): 1168-1170.
[2] Mayers R M, Butlin R J, Kilgour E, 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. Biochemical Society Transactions, 2003, 31(6): 1165-1167.