产品
编 号：F011798
分子式：C24H22ClN3O2
分子量：419.9
分子式：C24H22ClN3O2
分子量：419.9
产品类型
规格
价格
是否有货
5mg
询价
询价
结构图
CAS No: 1023650-66-9
产品详情
生物活性：
PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM.
体内研究：
PF-3882845 reduces blood pressure, decreases urinary albumin, and protects kidney in Dahl SS rat. PF-3882845 exhibits moderate oral bioavailability (F 86%) following oral administration (2 mg/kg) in male Sprague-Dawley rats.PF-3882845 exhibits terminal elimination half-lives (T1/2 1.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (Vdss 1.4 mL/kg respectively) following intravenous administration (2 mg/kg) in male Sprague-Dawley rats.Animal Model:Male Dahl salt sensitive (SS) rats
Dosage:10, 40, and 100 mg/kg
Administration:Orally via gavage; twice a day; for 21 days
Result:Significant blood pressure reduction was observed with 10 mg/kg. Most noticeably, rats dosed at 40 and 100 mg/kg had negligible increase in blood pressure over 21 days in the presence of high salt.
PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM.
体内研究：
PF-3882845 reduces blood pressure, decreases urinary albumin, and protects kidney in Dahl SS rat. PF-3882845 exhibits moderate oral bioavailability (F 86%) following oral administration (2 mg/kg) in male Sprague-Dawley rats.PF-3882845 exhibits terminal elimination half-lives (T1/2 1.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (Vdss 1.4 mL/kg respectively) following intravenous administration (2 mg/kg) in male Sprague-Dawley rats.Animal Model:Male Dahl salt sensitive (SS) rats
Dosage:10, 40, and 100 mg/kg
Administration:Orally via gavage; twice a day; for 21 days
Result:Significant blood pressure reduction was observed with 10 mg/kg. Most noticeably, rats dosed at 40 and 100 mg/kg had negligible increase in blood pressure over 21 days in the presence of high salt.
产品资料
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