1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. Mineralocorticoid Receptor Progesterone Receptor
  3. PF-3882845

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。

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PF-3882845 Chemical Structure

PF-3882845 Chemical Structure

CAS No. : 1023650-66-9

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规格 价格 是否有货 数量
5 mg ¥2549
3 - 4 周
10 mg   询价  
50 mg   询价  

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  • 生物活性

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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[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 (T1/2 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PF-3882845
目录号:
HY-12738
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