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Finerenone {[allProObj[0].p_purity_real_show]}

货号:A227647 同义名: BAY 94-8862;FIN Ambeed 开学季,买赠积分,赢豪礼

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

Finerenone 化学结构 CAS号:1050477-31-0
Finerenone 化学结构
CAS号:1050477-31-0
Finerenone 3D分子结构
CAS号:1050477-31-0
Finerenone 化学结构 CAS号:1050477-31-0
Finerenone 3D分子结构 CAS号:1050477-31-0
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Finerenone 纯度/质量文件 产品仅供科研

货号:A227647 标准纯度: {[allProObj[0].p_purity_real_show]}
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Finerenone 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].

Finerenone 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.

Finerenone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.21mL

2.64mL

1.32mL

26.43mL

5.29mL

2.64mL

Finerenone 技术信息

CAS号1050477-31-0
分子式C21H22N4O3
分子量 378.424
别名 BAY 94-8862;FIN
运输蓝冰
存储条件

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

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 190 mg/mL(502.08 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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