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Finerenone

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Chemical Structure| 1050477-31-0 同义名 : BAY 94-8862;FIN
CAS号 : 1050477-31-0
货号 : A227647
分子式 : C21H22N4O3
纯度 : 99%+
分子量 : 378.424
MDL号 : MFCD29047135
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：
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].
实验方案
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
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.