Eplerenone(Epoxymexrenone CGP 30083)

Molecular Weight (MW)	414.49
Formula	C24H30O6
CAS No.	107724-20-9
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 4 mg/mL (9.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)	Chemical Name: methyl (4aS,4bR,5aR,6aS,7R,9aS,9bR,10R)-4a,6a-dimethyl-2,5'-dioxo-2,4,4a,4',5a,5',6,6a,8,9,9a,9b,10,11-tetradecahydro-3H,3'H-spiro[cyclopenta[1,2]phenanthro[4,4a-b]oxirene-7,2'-furan]-10-carboxylate InChi Key: JUKPWJGBANNWMW-VWBFHTRKSA-N InChi Code: InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1 SMILES Code: C[C@]12CCC(C=C1C[C@@H](C(OC)=O)[C@@H]3[C@]24[C@@H](C[C@@]5(C)[C@H]3CC[C@@]56CCC(O6)=O)O4)=O
Synonyms	CGP-30083, SC-66110; CGP30083; CGP 30083; SC 66110; SC66110; Inspra; Selara

Molecular Weight (MW)

414.49

Formula

C24H30O6

CAS No.

107724-20-9

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 4 mg/mL (9.7 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In vivo)

Chemical Name: methyl (4aS,4bR,5aR,6aS,7R,9aS,9bR,10R)-4a,6a-dimethyl-2,5'-dioxo-2,4,4a,4',5a,5',6,6a,8,9,9a,9b,10,11-tetradecahydro-3H,3'H-spiro[cyclopenta[1,2]phenanthro[4,4a-b]oxirene-7,2'-furan]-10-carboxylate

InChi Key: JUKPWJGBANNWMW-VWBFHTRKSA-N

InChi Code: InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1

SMILES Code: C[C@]12CCC(C=C1C[C@@H](C(OC)=O)[C@@H]3[C@]24[C@@H](C[C@@]5(C)[C@H]3CC[C@@]56CCC(O6)=O)O4)=O

Synonyms

CGP-30083, SC-66110; CGP30083; CGP 30083; SC 66110; SC66110; Inspra; Selara

In Vitro	In vitro activity: N/A Kinase Assay: N/A Cell Assay: N/A
In Vivo	Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. Eplerenone increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. Eplerenone significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. Eplerenone increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. Eplerenone significantly decreases LV end-diastolic wall stress in dogs. Eplerenone is associated with a 28% reduction in cardiomyocyte cross-sectional area, a 37% reduction of volume fraction of reactive interstitial fibrosis, and a 34% reduction of volume fraction of replacement fibrosis in dogs with heart failure. Eplerenone blunts the increase in pulse pressure in Aldo rats and normalized Einc-wall stress curves, medial cross-sectional area (MCSA), and EIIIA fibronectin in aldosterone (Aldo)-salt hypertensive rats.
Animal model	Rats
Formulation & Dosage
References	Hypertension. 2005 Apr;45(4):538-44; J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63; Circulation. 2001 Jul 24;104(4):467-72.

In Vitro

In vitro activity: N/A

Kinase Assay: N/A

Cell Assay: N/A

In Vivo

Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. Eplerenone increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. Eplerenone significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. Eplerenone increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. Eplerenone significantly decreases LV end-diastolic wall stress in dogs. Eplerenone is associated with a 28% reduction in cardiomyocyte cross-sectional area, a 37% reduction of volume fraction of reactive interstitial fibrosis, and a 34% reduction of volume fraction of replacement fibrosis in dogs with heart failure. Eplerenone blunts the increase in pulse pressure in Aldo rats and normalized Einc-wall stress curves, medial cross-sectional area (MCSA), and EIIIA fibronectin in aldosterone (Aldo)-salt hypertensive rats.

Animal model

Rats

Formulation & Dosage

References

Hypertension. 2005 Apr;45(4):538-44; J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63; Circulation. 2001 Jul 24;104(4):467-72.

CAS NO:	107724-20-9
规格:	≥98%

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议