PF-3882845

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PF-3882845

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1023650-66-9

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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 (T_1/21.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (V_dss1.4 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.

分子量

419.90

Formula

C₂₄H₂₂ClN₃O₂

CAS 号

1023650-66-9

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.