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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Mineralocorticoid Receptor (MLR)-CS-3150
CS-3150

Chemical Structure : CS-3150

CAS No.: 1632006-28-0

CS-3150 (Esaxerenone, XL-550)

货号: PC-60739Not For Human Use, Lab Use Only.

CS-3150 (Esaxerenone, XL-550) is a highly potent, selective and orally active non-steroidal mineralocorticoid receptor antagonist with IC50 of 9.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CS-3150 (Esaxerenone, XL-550) is a highly potent, selective and orally active non-steroidal mineralocorticoid receptor (MR) antagonist with IC50 of 9.4 nM.
CS-3150 (Esaxerenone, XL-550) displays >1,000-fold selectivity over other steroid hormone receptors, glucocorticoid receptor, androgen receptor and progesterone receptor.
CS-3150 (Esaxerenone, XL-550) inhibits aldosterone-induced transcriptional activation of human mineralocorticoid receptor with IC50 of 3.7 nM.
CS-3150 (Esaxerenone, XL-550) shows superior potency to that of spironolactone and eplerenone; suppresses aldosterone-induced decrease in urinary Na(+)/K(+) ratio, inhibits blood pressure elevation induced by DOCA/salt-loading in rats.

物理化学性质&存储条件

分子量 466.475
分子式 C22H21F3N2O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-(2-Hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl) phenyl]-5-[2-(trifluoromethyl) phenyl]-1H-pyrrole-3-carboxamide

参考文献

1. Arai K, et al. Eur J Pharmacol. 2015 Aug 15;761:226-34.

2. Arai K, et al. Eur J Pharmacol. 2015 Dec 15;769:266-73.

3. Arai K, et al. J Pharmacol Exp Ther. 2016 Sep;358(3):548-57.

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