产品说明书
AZD7545
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同义名 : | - |
| CAS号 : | 252017-04-2 | |
| 货号 : | A349552 | |
| 分子式 : | C19H18ClF3N2O5S | |
| 纯度 : | 99%+ | |
| 分子量 : | 478.87 | |
| MDL号 : | MFCD25976792 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 45 mg/mL(93.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 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] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.44mL 2.09mL 1.04mL |
20.88mL 4.18mL 2.09mL |
| 参考文献 |
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