China (Mainland)
Eplerenone CAS NO.107724-20-9
- Min.Order: 1 Metric Ton
- Payment Terms: T/T,
- Product Details
Keywords
- Eplerenone
- 55079-83-9
Quick Details
- ProName: Eplerenone
- CasNo: 107724-20-9
- Appearance: white powder
- DeliveryTime: 3 days after payment
- PackAge: 25kg/plastic drum,200Kg/iron drum
- Port: Shanghai, Shenzhen, Guangzhou, Hongkon...
- ProductionCapacity: 1 Metric Ton/Day
- Purity: 99%
- Storage: Keep in cool and dry place, away from ...
- LimitNum: 1 Metric Ton
- Related Substances: <0.1%
- Residue on Ignition: <0.1%
- Heavy Metal: <0.002%
- Valid Period: 2 years
Superiority
Details
- 【Specification】
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?Eplerenone (CAS NO.107724-20-9), its Synonyms are 9,11alpha-Epoxy-17-hydroxy-3-oxo-17alpha-pregn-4-ene-7alpha,21-dicarboxylic acid, gamma-lactone, methyl ester ; Epoxymexrenone ; Inspra ; Pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo-, gamma-lactone, methyl ester, (7alpha,11alpha,17alpha)- .
Biomedical Effects and Toxicity
- 【Biological Activity】
- 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 .
- 【Pharmacological Action】
- - Compounds which inhibit or antagonize the biosynthesis or actions of aldosterone.
- 【Therapeutic Uses】
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Eplerenone is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive drugs. /Included in US product labeling/
Inspra is indicated to improve survival of stable patients with left ventricular systolic dysfunction (ejection fraction less than or equal to 40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.
... Eplerenone should replace spironolactone as a natriuretic and antikaliuretic in heart failure and as add-on treatment in severe systolic cardiac insufficiency, and it is indicated after an acute myocardial infarction complicated by left ventricular dysfunction and heart failure. The finding that hypertension control with diuretic-based pharmacotherapy results in better prevention of heart failure than pressure reduction with other drugs makes it pertinent to investigate whether diuretics in general, and eplerenone in particular, should constitute part of the initial pharmacotherapy for heart failure when there is no overt fluid retention and independent of the etiology. ... [Reyes AJ et al; Eur J Intern Med 16 (1): 3-11 (2005)]
- 【Biomedical Effects and Toxicity】
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Apparent plasma clearance: approximately 10 L/hr. Less than 5% is recovered as unchanged drug in the urine and feces. Renal: 67%. Fecal: 32%.
Mean peak plasma concentrations of eplerenone are reached approximately 1.5 hours following oral administration. The absolute bioavailability of eplerenone is unknown. Both peak plasma levels (Cmax) and area under the curve (AUC) are dose proportional for doses of 25 to 100 mg and less than proportional at doses above 100 mg. The plasma protein binding of eplerenone is about 50% and it is primarily bound to alpha 1-acid glycoproteins. The apparent volume of distribution at steady state ranged from 43 to 90 L. Eplerenone does not preferentially bind to red blood cells.
Eplerenone is distributed into milk in rats; ... .
... Preclinical data show that eplerenone and/or metabolites are present in rat breast milk (0.85:1 [milk:plasma] AUC ratio) obtained after a single oral dose. Peak concentrations in plasma and milk were obtained from 0.5 to 1 hour after dosing.