PF-06409577
| CAS号 | 1467057-23-3 | 货号 | BCP32554 |
| 中文名 | PF-06409577 | ||
| 英文名 | PF-06409577 | ||
| 中文别名 | |||
| 英文别名 | PF06409577; PF 06409577; PF-6409577; PF6409577; PF 6409577; | ||
| 分子式 | C19H16ClNO3 | 分子量 | 341.79 |
| 生物活性 | PF-06409577 is a potent and selective activator of 5′ adenosine monophosphate-activated protein kinase (AMPK) for the Potential Treatment of diabetic nephropathy. PF-06409577 has AMPK α1β1γ1 Kd=9.0 nM. AMPK α1β1γ1 EC50 = 7.0 nM; AMPK α1β2γ1 EC50 > 40000 nM. PF-06409577 showed efficacy in a preclinical model of diabetic nephropathy. Upon the basis of its potent and selective AMPK activation, low metabolic turnover in human hepatocytes, clean off-target profile, and favorable preclinical in vivo efficacy results, PF-06409577 was profiled in regulatory toxicology studies and was subsequently advanced to clinical trials to assess human pharmacokinetics and safety/ tolerability. | ||
| 信号通路 | PI3K/Akt/mTOR Epigenetics | ||
| 靶 点 | AMPK | ||
结构式
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