Eprosartan (mesylate)

Angiotensin II, as part of the renin-angiotensin-aldosterone system, facilitates a sympathetic nervous system response mediated by the angiotensin II type 1 (AT1) receptor, causing vasoconstriction and subsequent increase in blood pressure. It potentiates noradrenaline release from sympathetic nerve terminals at the presynaptic level as well as amplifies the alpha-adrenoceptor-mediated vasoconstrictor response to endogenous noradrenaline. Angiotensin II receptor blockers (ARBs) are a major class of therapeutics designed to lower blood pressure and to provide cardiovascular protection. Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 - 3.9 nM and an elimination half-life of five to seven hours. Eprosartan is structurally distinct from other noncompetitive ARBs in that it does not contain a biphenyl, tetrazole moiety and blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.Formal Name: (alphaE)-[[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene]-2-thiophenepropanoic acid, mesylate. CAS Number: 144143-96-4. Synonyms: SKF 108566J. Molecular Formula: C23H24N2O4S . CH3SO3H. Formula Weight: 520.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 233, 271 nm. SMILES: CCCCC1=NC=C(/C=C(CC2=CC=CS2)/C(O)=O)N1CC3=CC=C(C(O)=O)C=C3.O=S(O)(C)=O. 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+,. InChi Key: DJSLTDBPKHORNY-XMMWENQYSA-N.