Eplerenone

한글명:Eplerenone

카스 번호107724-20-9

상품명:Eplerenone

CBNumberCB3489802

분자식C24H30O6

포뮬러 무게414.49

MOL 파일107724-20-9.mol

화학적 성질

녹는점	241-243°C
알파	D +5° (c = 0.437 in chloroform)
끓는 점	597.9±50.0 °C(Predicted)
밀도	1.31±0.1 g/cm3(Predicted)
저장 조건	Store at RT
용해도	DMSO: 용해성2mg/mL, 투명(가온)
물리적 상태	가루
색상	흰색에서 베이지색
최대 파장(λmax)	240nm(lit.)
Merck	14,3625
InChIKey	UZZAHAKTLYRDOK-MGIDJNSKSA-N
SMILES	[C@@]123[C@@]4(C)CCC(=O)C=C4C[C@@H](C(OC)=O)[C@@]1([H])[C@]1([H])CC[C@]4(CCC(=O)O4)[C@]1(C[C@@]2([H])O3)C \|&1:0,1,10,15,17,21,27,29,r\|

위험 및 안전 성명

유엔번호(UN No.)	3077
WGK 독일	3
HS 번호	29322090
유해 물질 데이터	107724-20-9(Hazardous Substances Data)

그림문자(GHS)

Eplerenone 화학적 특성, 용도, 생산

개요
Eplerenone is a mineralocorticoid receptor antagonist. It is selective for the mineralocorticoid receptor over glucocorticoid, androgen, progesterone, and estrogen receptors in radioligand binding assays (IC₅₀s = 138, 6,920, 523, >10,000, and 5,702 nM, respectively). Eplerenone inhibits aldosterone-induced mineralocorticoid activity in a luciferase assay (IC₅₀ = 122 nM). In vivo, eplerenone (100 mg/kg per day) reduces urinary albumin secretion and glomerulosclerosis in the Dahl salt-sensitive rat model of hypertension and nephropathy. It reduces myocardial IL-1β levels and collagen deposition, as well as improves left ventricular systolic dysfunction in a mouse model of acute myocardial infarction. Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.
화학적 성질
White Solid
용도
Selective aldosterone receptor antagonist (SARA), structurally similar to Spiranolactone. Eplerenone is used alone or in combination with other medications to treat high blood pressure. Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. It works by blocking the action of aldosterone, a natural substance in the body that raises blood pressure.
일반 설명
Eplerenone, 9,11α-epoxy-17α-hydroxy-3-oxopregn-4-ene-7α,21-dicarboxylic acid, γ-lactone,methyl ester (Inspra), is a newer aldosterone antagonist that isused for the treatment of hypertension.
생물학적 활성
Selective mineralocorticoid (aldosterone) receptor antagonist (IC 50 = 360 nM). Displays > 27-fold selectivity over androgen, progesterone and estrogen receptors (IC 50 > 10 μ M). Orally active antihypertensive in vivo .
Clinical Use
A newer drug, eplerenone, has a structure similar to that of spironolactone and a similar mechanism of action. It was initially approved for use in the treatment of hypertension but it can now be used in the treatment of patients with left ventricular systolic dysfunction and congestive heart failure after myocardial infarction.

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