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Eprosartan mesylate(SKF-108566J)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eprosartan mesylate(SKF-108566J)图片
CAS NO:144143-96-4
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)520.62
FormulaC23H24N2O4S.CH4O3S
CAS No.144143-96-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 104 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.7 mM)
Other info

Chemical Name: 4-[[2-butyl-5-[(E)-2-carboxy-3-thiophen-2-ylprop-1-enyl]imidazol-1-yl]methyl]benzoic acid;methanesulfonic acid

InChi Key: DJSLTDBPKHORNY-XMMWENQYSA-N

InChi Code: InChI=1S/C23H24N2O4S.CH4O3S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27;1-5(2,3)4/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29);1H3,(H,2,3,4)/b18-12+;

SMILES Code: CCCCC1=NC=C(N1CC2=CC=C(C=C2)C(=O)O)/C=C(\CC3=CC=CS3)/C(=O)O.CS(=O)(=O)O

Synonyms

SKF-108566; SKF108566; SKF 108566; Teveten; Futuran; Navixen; Regulaten; SK and F 108566;

实验参考方法
In Vitro

In vitro activity: Eprosartan inhibits [125I]-angiotensin II binding with IC50 1.4 nM to 3.9 nM in human tissues (adrenal cortex, liver, cloned AT1 receptor) and 1.5 nM to 9.2 nM in rat tissues (e.g. mesenteric artery, adrenal cortex, renal glomerulus). Eprosartan (100 nM), but not an AT2 antagonist, completely blocks angiotensin II-induced isotonic fluid absorption in rabbit isolated perfused proximal convoluted tubules.

In VivoEprosartan (3 mg/kg-10 mg/kg, administered by duodenal or gastric catheter) also produces a dose-dependent inhibition of the pressor response to angiotensin II in conscious normotensive rats. Eprosartan (10 mg/kg) dose-dependently reduces blood pressure and antihypertensive activity is maintained for 1.5 hours in renin-dependent hypertensive rats. Eprosartan (60 mg/kg/day, intraperitoneally) is associated with no mortality (0 of 20 rats) after 18 weeks compared with a 100% mortality rate by week 9 among 20 vehicle-treated rats. Eprosartan (10 mg/kg) dose-dependently reduces mean arterial pressure and does not cause reflex tachycardia in dogs. Eprosartan (0.3 mg/kg) inhibits the pressor response induced by electronic stimulation of the spinal cord in the pithed rat. Eprosartan inhibits amino acid-induced glomerular hyperfiltration in rats. Eprosartan (0.3 mg/kg i.v.) inhibits the pressor response induced by spinal cord stimulation in a manner similar to that observed with the peptide antagonist, Sar1, Ile8[angiotensin II] in the pithed rat. Eprosartan is more effective in inhibiting sympathetic nervous system activity compared to other chemically distinct nonpeptide angiotensin II receptor antagonists.
Animal modelRats
Formulation & Dosage3 mg/kg-10 mg/kg, administered by duodenal or gastric catheter
References

Drugs. 2000 Jul;60(1):177-201; Pharmacology. 1997 Nov;55(5):244-51.