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KI1416Eplerenone10 mg$154
Eplerenone25 mg$272

Chemical Characteristic

Product NameEplerenone
SynonymsInspra
CAS No.107724-20-9
Molecular Weight 414.49
FormulaC24H30O6
Chemical Name(7?,?11?,?17?)?-9,?11-?epoxy-?17-?hydroxy-?3-?oxo-??-?lactone-pregn-?4-?ene-?7,?21-?dicarboxylic acid-7-?methyl ester
SmilesC1C(=O)C=C2[C@](C1)([C@]13[C@@H]([C@@H](C2)C(=O)OC)[C@H]2[C@](C[C@H]1O3)([C@@]1(CC2)OC(=O)CC1)C)C
Chemical Structure

Biological activities

Eplerenone is a selective aldosterone receptor blocker. The IC50 of eplerenone is 360 nM against aldosterone receptor.[1] Eplerenone increases sodium concentration from 135 to 145 mM in endothelial cells0.[2] Eplerenone inhibits the increased phosphorylation of OSR1 and NCC in the mouse kidney. [3] Eplerenone produces significant cardioprotective effects in experimental models of cardiovascular disease.[4] It is reported that eplerenone prevents L-NAME/Angiotensin II-induced renal injury in rats. [5]

Protocols

In vitro: Eplerenone is dissolved in ethanol.[2]

References

[1] George J, et al. Evaluation of the aldosterone-blocking agent eplerenone in hypertension and heart failure. Expert Opin Pharmacother. 2007, 8(17): 3053-3059.
[2] Oberleithner H, et al. Plasma sodium stiffens vascular endothelium and reduces nitric oxide release. Proc Natl Acad Sci. 2007, 104(41): 16281-16286.
[3] Talati G, et al. Effect of angiotensin II on the WNK-OSR1/SPAK-NCC phosphorylation cascade in cultured mpkDCT cells and in vivo mouse kidney. Biochem Biophys Res Commun. 2010, 393(4): 844-848.
[4] McMahon EG. et al. Recent studies with eplerenone, a novel selective aldosterone receptor antagonist. Curr Opin Pharmacol. 2001, 1(2): 190-196.
[5] John W. et al. Eplerenone, a new mineralocorticoid antagonist:in vitro and in vivo studies. Current Opinion in Endocrinology & Diabetes. 2000, 7(3): 138-142

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