EplerenoneAn MCR antagonist

Eplerenone (CAS 107724-20-9)

Eplerenone | CAS 107724-20-9 is rated 5.0 out of 5 by 1.
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Synonym: Inspra; Epoxymexrenone; 9,11alpha-Epoxy-17-hydroxy-3-oxo-17alpha-pregn-4-ene-7alpha,21-dicarboxylic acid
Application: An MCR antagonist
CAS Number: 107724-20-9
Purity: >99%
Molecular Weight: 414.49
Molecular Formula: C24H30O6
* Refer to Certificate of Analysis for lot specific data (including water content).
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Eplerenone is an aldosterone antagonist with more specificity for the mineralocorticoid receptor (MCR) than spironolactone (sc-204294), having lower affinity for progesterone, androgen, and glucocorticoid receptors.


References

De Gasparo et al (1987) Three new epoxy-spirolactone derivatives: characterization in vivo and in vitro. J.Pharmacol.Exp.Ther. 240 650. McMahon (2001) Recent studies with eplerenone, a novel selective aldosterone receptor antagonist. Curr.Opin.Pharmacol. 1 190.

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (10 mM), water (very slightly), ethanol (slightly), methanol (sparingly), and chloroform.
Storage :
Store at room temperature
Melting Point :
>219° C
Boiling Point :
597.93° C at 760 mmHg (Predicted)
Density :
1.31 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
Optical Activity :
α20/D +2.7°, c = 0.44 in chloroform
IC50 :
MCR: IC50 = 81 nM; MCR: IC50 = 122 nM (human); MCR: IC50 = 0.36 µM; GR: IC50 >8.94 µM (human); PR: IC50 >10 µM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
TU4814000
PubChem CID :
443872
SMILES :
CC12CCC(=O)C=C1CC(C3C24C(O4)CC5(C3CCC56CCC(=O)O6)C)C(=O)OC

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Certificate of Analysis

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Eplerenone  Product Citations

See how others have used Eplerenone. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 23085982  Rudmann, DG. et al. 2013. Toxicol Pathol. 41: 310-4.

PMID: # 17023667  Ohtani, T. et al. 2007. Am. J. Physiol. Regul. Integr. Comp. Physiol. 292: R946-R954.

PMID: # 16901964  Guo, C. et al. 2006. Endocrinology. 147(11): 5363-5373.

Citations 1 to 3 of 3 total

What is the solubility of the compound?

Asked by: two2igm05
Thank you for your question. The solubility for sc-203943 is as follows: DMSO 4mg/mL (9.65 mM) warming, Water <1mg/mL, and Ethanol <1mg/mL. If you have any further questions or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing scbt@scbt.com, or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-01-12
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Rated 5 out of 5 by from Ohtani Ohtani, T. et al. (PubMed 17023667) used eplerenone, a selective mineralocorticoid receptor antagonist, on Dahl salt-sensitive rats exhibiting diastolic heart failure (DHF). Introduction of eplerenone led to prevention of overt DHF by blockade of the mineralocorticoid receptor. -SCBT Publication Review
Date published: 2015-04-06
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