Eplerenone|107724-20-9|(依普利酮; Epoxymexrenone)-陌孚医药/Medlife

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Eplerenone (Synonyms: 依普利酮; Epoxymexrenone)

目录号: PL07293 纯度: ≥99%

CAS No. :107724-20-9

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中文名称	Eplerenone
中文别名	依普利酮;伊普利酮;6-(三丁基锡)-3-吡啶甲醛;Eplerenone 依普利酮;雌三醇;依普黄酮;依普利酮 USP标准品;依普利酮,In-house Standard;依普利酮-13C-D3;依普利酮-D3;9,11α-乙氧基-17-羟基-3-氧-17α-孕-4-烯-7α,21-二羧酸-γ-内甲酯;普利酮;埃普利酮;依普利酮(标准品);依普利酮, 选择性盐皮质激素受体拮抗剂;依普利酮(伊普利酮、依普利酮-13C-D3、普利酮)
英文名称	Eplerenone
英文别名	eplerenone;(7A,11A,17A)-9,11-EPOXY-17-HYDROXY-3-OXO-PREGN-4-ENE-7,21-DICARBOXYLIC ACID G-LACTONE METHYL ESTER;pregn-4-ene-7,21-dicarboxylic acid 9,11-epoxy-17-hydroxy-3-oxo gamma-lactone methyl ester;EPLERENONE USP STANDARD;EplerenoneC24H3006;(2'R,4aS,4bR,5aR,6aS,9aS,9bR,10R)-methyl 4a,6a-dimethyl-2,4'-dioxo-3,4,4a,4',5a,5',6,6a,8,9,9a,9b,10,11-tetradecahydro-2H,3'H-spiro[cyclopenta[1,2]phenanthro[4,4a-b]oxirene-7,2'-furan]-10-carboxylate;ALTINICLINE;Eplerenone (SC-66110, ,CGP30083, Epoxymexrenone,Inspra®, );Epoxymexrenone;9,11α-Epoxy-17-hydroxy-3-oxo-17α-pregn-4-ene-7α,21-dicarboxylic Acid γ-Lactone Methyl Ester;Elperenone;Epleremone;EPLERINONE;Inspra;9,11alpha-Epoxy-17-hydroxy-3-oxo-17alpha-pregn-4-ene-7alpha,21-dicarboxylic acid, gamma-lactone, methyl ester;Cgp 30083;Eplerenone [USAN];HSDB 7522;Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-, gamma-lactone, methyl ester, (7alpha,11alpha,17alpha)-;SC-66110;Eplerenone-13C-d3;EPLERENONE 98%;Selara;6995V82D0B;DSSTox_RID_81333;DSSTox_CID_26094;DSSTox_GSID_46094;(+)-Eplerenone;Inspra (TN)
Cas No.	107724-20-9
分子式	C₂₄H₃₀O₆
分子量	414.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Eplerenone (Epoxymexrenone) 是一种选择性和高度特异性醛固酮阻滞剂 (SAB)，具有口服活性。Eplerenone 也是一种选择性矿糖皮质激素受体拮抗剂 (MRA)，其 IC₅₀ 值为 0.081 μM。Eplerenone 可用于高血压、动脉粥样硬化、慢性收缩期心力衰竭 (HF) 和心血管 (CV) 的研究。

生物活性

Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC 50 value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV).

性状

Solid

IC50 & Target[1][2]

IC50: 0.081 μM (human mineralocorticoid receptor)

体外研究(In Vitro)

Eplerenone inhibits the human mineralocorticoid receptor with IC50 value of 0.081 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Eplerenone (oral, 200 mg/kg/day for 3 months) significantly reduces oxidative stress and atherosclerosis progression in atherosclerotic apolipoprotein edeficient (EO) mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Myron H Weinberger, et al. Eplerenone, a selective aldosterone blocker, in mild-to-moderate hypertension. Am J Hypertens. 2002 Aug;15(8):709-16.
[2]. Dhillon, S., Eplerenone: a review of its use in patients with chronic systolic heart failure and mild symptoms. Drugs, 2013. 73(13): p. 1451-62.
[3]. Shlomo Keid

溶解度数据	In Vitro: DMSO : 25 mg/mL (60.32 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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