PF-3882845 是一种高亲和力的,口服有效的选择性盐皮质激素受体 (MR; 结合IC50=2.7 nM) 拮抗剂,有潜力用于高血压和肾病的研究。PF-3882845 还与孕激素受体 (PR) 结合,结合IC50为 310 nM。
生物活性 | PF-3882845 is a remarkably high affinity selective and orally efficaciousmineralocorticoid receptor(MRbindingIC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds toprogesterone receptor(PR) with the bindingIC50of 310 nM[1]. |
IC50& Target | IC50: 2.7 nM (mineralocorticoid receptor), 310 nM (progesterone receptor)[1] |
体内研究 (In Vivo) | PF-3882845 reduces blood pressure, decreases urinary albumin, and protects kidney in Dahl SS rat[1]. PF-3882845 exhibits moderate oral bioavailability (F 86%) following oral administration (2 mg/kg) in male Sprague-Dawley rats[1]. PF-3882845 exhibits terminal elimination half-lives (T1/21.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (Vdss1.4 mL/kg respectively) following intravenous administration (2 mg/kg) in male Sprague-Dawley rats[1].
Animal Model: | Male Dahl salt sensitive (SS) rats[1] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |