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CAS No.: 252017-04-2

AZD7545 Catalog No. CSN13656

Synonyms: AZD7545

AZD7545 is a selective inhibitor of PDHK2 (PDH kinase2) with IC50s of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.

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实验方案

技术信息

生物活性

描述PDHK (pyruvate dehydrogenase kinase) is a kinase enzyme which acts to inactivate the enzyme pyruvate dehydrogenase by phosphorylating it using ATP. AZD7545 is a novel PDHK inhibitor with IC50 values of 36.8nM/6.4nM for PDHK1/2^[3], and EC50 value of 5.2nM for increasing PDH activity. It stimulated the rate of pyruvate oxidation with EC50 value of 105nM in rat hepatocytes. A single dose of AZD7545 to Wistar rats increased the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner from 24.7 to 70.3% at 30 mg/kg; and in skeletal muscle from 21.1 to 53.3%. A single dose of 10 mg/kg also significantly elevated muscle PDH activity in obese Zucker (fa/fa) rats. AZD7545 (10 mg/kg) twice daily for 7 days markedly improved the 24-h glucose profile, by eliminating the postprandial elevation in blood glucose^[4]. AZD7545 failed to inhibit PDHK4 and paradoxically, at higher concentrations (>10 nM), AZD7545 stimulated PDHK4 activity^[3].
作用机制AZD7545 docks into the lipoamide-binding site on PDHK2 thus inhibiting interaction with the E2 subunit. It inhibits PDHK in a non-ATP competitive manner.^[3]
动物研究
剂量
Rat: 10 mg/kg - 30 mg/kg^[2] (p.o.), 300 mg/kg^[3] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Rat: 10 mg/kg - 30 mg/kg^[2] (p.o.), 300 mg/kg^[3] (p.o.)
给药途径	p.o.

[1] Morrell JA, Orme J, 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, Butlin RJ, 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.
[3] Morrell JA, Orme J, Butlin RJ, Roche TE, Mayers RM, Kilgour E. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70. doi: 10.1042/bst0311168. PMID: 14641019.
[4] Mayers RM, Butlin RJ, Kilgour E, Leighton B, Martin D, Myatt J, Orme JP, Holloway BR. 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. doi: 10.1042/bst0311165. PMID: 14641018.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0883 mL
- 10.4413 mL
- 20.8825 mL
- 5 mM
- 0.4177 mL
- 2.0883 mL
- 4.1765 mL
- 10 mM
- 0.2088 mL
- 1.0441 mL
- 2.0883 mL

技术信息

CAS号

252017-04-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18ClF3N2O5S

运输

蓝冰

分子量

478.87

别名

AZD7545

溶解度

DMSO	95.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	95.0 mg/mL (198.4 mM)

动物实验配方

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AZD7545 Catalog No. CSN13656

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