PF-3882845 NLT 98%

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^[1]. IC50 & Target: IC50: 2.7 nM (mineralocorticoid receptor), 310 nM (progesterone receptor)^[1] 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 (T_1/2 1.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (V_dss 1.4 mL/kg respectively) following intravenous administration (2 mg/kg) in male Sprague-Dawley rats^[1].