top Eplerenone

top Eplerenone

top Eplerenone

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1 Gram

FOB Price: USD 1.0000

  • Min.Order :1 Gram
  • Purity: 99% min
  • Payment Terms : L/C,T/T,

Keywords

Eplerenone high purity Eplerenone factory supply Eplerenone

Quick Details

  • Appearance:white to light yellow crystal powder
  • Application:Pharmaceutical intermediates
  • PackAge:as you requested
  • ProductionCapacity:10|Kilogram|Day
  • Storage:Room temperature
  • Transportation:by courier

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Details:

Product Name: Eplerenone
Synonyms: pregn-4-ene-7,21-dicarboxylic acid 9,11-epoxy-17-hydroxy-3-oxo gamma-lactone methyl ester;EPLERENONE 98%;EPLERENONE USP STANDARD;Elperenone;EplerenoneC24H3006;pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7 α, 11 α, 17 α);EPLERENONE AND N-1 INTERMEDIATE;epoxymexrenone
CAS: 107724-20-9
MF: C24H30O6
MW: 414.49
EINECS:  
Product Categories: Antihypertensive;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Steroids;Steroid and Hormone;Inspra;Cardiovascular APIs
Mol File: 107724-20-9.mol
Eplerenone Structure
 
Eplerenone Chemical Properties
Melting point  241-243°C
alpha  D +5° (c = 0.437 in chloroform)
storage temp.  Store at RT
solubility  DMSO: soluble2mg/mL, clear (warmed)
color  white to beige
λmax 240nm(lit.)
Merck  14,3625
 
Safety Information
RIDADR  3077
Hazardous Substances Data 107724-20-9(Hazardous Substances Data)
MSDS Information
 
 
Eplerenone Usage And Synthesis
Overview Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. It can be used individually or in combination with other medications to treat hypertension by blocking the action of aldosterone, a natural substance in the body that raises blood pressure.
Chemical properties Eplerenone is an odorless, white to off-white crystalline powder. It is very slightly soluble in water, with its solubility essentially pH-independent. The octanol/water partition coefficient of eplerenone is approximately 7.1 at pH 7.0.
Mechanism of action Aldosterone,with many physiological and pathological effects, can cause central blood pressure and endothelial injury (catecholamines enhance its role), reduce heart rate variability, induce ventricular arrhythmias, and promote retention of sodium, potassium and magnesium loss, promote myocardial fibrosis, necrosis and inflammation, damage the fibrinolytic system.
Angiotensin converting enzyme inhibitors (also called angiotensin converting enzyme inhibitors, referred to as ACEI) and angiotensin Ⅱ receptor antagonist ARB aldosterone can inhibit the secretion of adrenaline, but after a period of treatment.The release of aldosterone was restored,which may even exceed the baseline plasma concentration levels. Despite adequate treatment of ACEI and ARB, aldosterone-induced damage can still happen, so it is necessary to use aldosterone receptor antagonists in the treatment of hypertension. Clinical studies have shown that patients who are not satisfied with the efficacy of ACEI or ARB therapy can add eplerenone along with the treatment.
Non-selective aldosterone receptor antagonist spironolactone can reduce mortality in patients with congestive heart failure, However, the side effects of male hyperplasia and other diseases associated with sex hormones have limited its application in the treatment of hypertension.
Adverse effects Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration.
References #
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Chemical Properties White Solid
Uses 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.
Uses Eplerenone is an aldosterone antagonist with an IC50 of 0.36 μM. It is used as an adjunct in the management of chronic heart failure. It is similar to the diuretic spironolactone, though it may be more specific for the mineralocorticoid receptor and is sp
Uses anticancer agent
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 .

 

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