| 包装: | 2.5mg |
| 规格: | 98% |
| 市场价: | 9261元 |
| 分子量: | 417.5 |
Background:
Eplerenone-d3is intended for use as an internal standard for the quantification of eplerenone by GC- or LC-MS. Eplerenone is a mineralocorticoid receptor antagonist.1It 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.2Formulations containing eplerenone have been used in the treatment of hypertension and heart failure after myocardial infarction.
1.Meyers, M.J., Arhancet, G.B., Hockerman, S.L., et al.Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathyJ. Med. Chem.53(16)5979-6002(2010) 2.Chen, B., Geng, J., Gao, S.-X., et al.Eplerenone modulates interleukin-33/sST2 signaling and IL-1β in left ventricular systolic dysfunction after acute myocardial infarctionJ. Interferon. Cytokine Res.38(3)137-144(2018)
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