CAS 133040-01-4|Eprosartan

Introduction:Basic information about CAS 133040-01-4|Eprosartan, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameEprosartan
CAS Number133040-01-4Molecular Weight424.513
Density1.3±0.1 g/cm3Boiling Point660.6±55.0 °C at 760 mmHg
Molecular FormulaC23H24N2O4SMelting Point250-253ºC
MSDS/Flash Point353.3±31.5 °C

Names

Nameeprosartan
SynonymMore Synonyms

Eprosartan BiologicalActivity

DescriptionEprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
Related CatalogResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>GPCR/G Protein >>Angiotensin Receptor
In VitroEprosartan (SKF-108566J) inhibits [125I]AII binding to human liver membranes (IC50 of 1.7 nM) and to rat mesenteric artery membranes (IC50 of 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[1].
In VivoIn conscious normotensive rats, i.v. administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr[1].
References

[1]. R M Edwards, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther. 1992 Jan;260(1):175-81.

Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point660.6±55.0 °C at 760 mmHg
Melting Point250-253ºC
Molecular FormulaC23H24N2O4S
Molecular Weight424.513
Flash Point353.3±31.5 °C
Exact Mass424.145691
PSA120.66000
LogP4.96
Vapour Pressure0.0±2.1 mmHg at 25°C
Index of Refraction1.628
InChIKeyOROAFUQRIXKEMV-LDADJPATSA-N
SMILESCCCCc1ncc(C=C(Cc2cccs2)C(=O)O)n1Cc1ccc(C(=O)O)cc1
Storage condition-20°C Freezer

Safety Information

Hazard CodesXi
Risk PhrasesR36/37/38
Safety PhrasesS26

Synonyms

2-Thiophenepropanoic acid, α-[[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene]-
MFCD08141807
4-({2-Butyl-5-[2-carboxy-3-(2-thienyl)-1-propen-1-yl]-1H-imidazol-1-yl}methyl)benzoic acid
Eprosartan
4-[[2-butyl-5-[(E)-2-carboxy-3-thiophen-2-ylprop-1-enyl]imidazol-1-yl]methyl]benzoic acid
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