Eprosartan

Modify Date: 2024-01-08 11:24:55

Eprosartan Structure
Eprosartan structure
Common Name Eprosartan
CAS Number 133040-01-4 Molecular Weight 424.513
Density 1.3±0.1 g/cm3 Boiling Point 660.6±55.0 °C at 760 mmHg
Molecular Formula C23H24N2O4S Melting Point 250-253ºC
MSDS N/A Flash Point 353.3±31.5 °C

 Use of Eprosartan


Eprosartan (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].

 Names

Name eprosartan
Synonym More Synonyms

 Eprosartan Biological Activity

Description Eprosartan (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 Catalog
In Vitro Eprosartan (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 Vivo In 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

Density 1.3±0.1 g/cm3
Boiling Point 660.6±55.0 °C at 760 mmHg
Melting Point 250-253ºC
Molecular Formula C23H24N2O4S
Molecular Weight 424.513
Flash Point 353.3±31.5 °C
Exact Mass 424.145691
PSA 120.66000
LogP 4.96
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.628
Storage condition -20°C Freezer

 Safety Information

Hazard Codes Xi
Risk Phrases R36/37/38
Safety Phrases S26

 Synthetic Route

 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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