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CAS No.: 1050477-31-0

Finerenone Catalog No. CSN29446

Synonyms: BAY 94-8862

Finerenone is a novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonist with IC50 value of 18nM.

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400-920-2911

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技术信息

生物活性

描述Excessive activation of mineralocorticoid receptors by the steroid hormones aldosterone or cortisol can lead to the development of cardiovascular disease. Finerenone is a novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonist with IC50 value of 18nM and exhibits no activity at any other steroid hormone receptor and on 65 receptors and ion channels (IC50>10μM). Finerenone showed a favorable PK profile and high oral bioavailability (94%) in rats^[1]. Finerenone reduced cardiac hypertrophy, plasma prohormone of brain natriuretic peptide, and proteinuria more efficiently than eplerenone when comparing equinatriuretic doses. It improved systolic and diastolic left ventricular function and reduced plasma prohormone of brain natriuretic peptide levels at dose of 1mg/kg, daily, p.o., in rats that developed chronic heart failure after coronary artery ligation, suggesting that finerenone may offer end-organ protection with a reduced risk of electrolyte disturbances^[2].
作用机制Finerenone fills part of the MR binding pocket between Asn770 and Leu766^[1].
参考文献

[1] Bärfacker L, Kuhl A, Hillisch A, Grosser R, Figueroa-Pérez S, Heckroth H, Nitsche A, Ergüden JK, Gielen-Haertwig H, Schlemmer KH, Mittendorf J, Paulsen H, Platzek J, Kolkhof P. Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases. ChemMedChem. 2012 Aug;7(8):1385-403. doi: 10.1002/cmdc.201200081. Epub 2012 Jul 12. PMID: 22791416.
[2] Kolkhof P, Delbeck M, Kretschmer A, Steinke W, Hartmann E, Bärfacker L, Eitner F, Albrecht-Küpper B, Schäfer S. Finerenone, a novel selective nonsteroidal mineralocorticoid receptor antagonist protects from rat cardiorenal injury. J Cardiovasc Pharmacol. 2014 Jul;64(1):69-78. doi: 10.1097/FJC.0000000000000091. PMID: 24621652.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6425 mL
- 13.2127 mL
- 26.4254 mL
- 5 mM
- 0.5285 mL
- 2.6425 mL
- 5.2851 mL
- 10 mM
- 0.2643 mL
- 1.3213 mL
- 2.6425 mL

技术信息

CAS号

1050477-31-0

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H22N4O3

运输

蓝冰

分子量

378.42

别名

BAY 94-8862

溶解度

DMSO	75.0 mg/mL (198.2 mM)

动物实验配方

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