Irbesartan , 2mMinDMSO , 138402-11-6

Synonym(s):
2-Butyl-3-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one;Avapro;BMS-186295;SR-47436

CAS NO.：138402-11-6

Empirical Formula: C25H28N6O

Molecular Weight: 428.53

MDL number: MFCD00864464

EINECS: 604-078-2

PRODUCT Properties

• Melting point: 180-181°C
• Boiling point: 648.6±65.0 °C(Predicted)
• Density: 1.30±0.1 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO: >25mg/mL
• pka: 4.16±0.10(Predicted)
• form: powder
• color: white to off-white
• Merck: 14,5083
• BCS Class: 2

Description and Uses

Avapro was launched in Germany, the UK and the US for hypertension. It can be prepared in six steps starting with cyclopentanone or in three steps from 1- aminocyclopentanecarboxylic acid ethyl ester and pentanimidic ethyl ester. Avapro is an angiotensin Ⅱ receptor antagonist that is non-competitive and selective for AT, subtypes and has no AT₂ activity at postsynaptic receptors compared to presynatpic. It has no affinity for various non angiotensin Ⅱ receptor types in binding, no interaction with calcium channels or antiports, and no affinity for α₁- and α₂--adrenoreceptors, serotonergic receptors, muscarinic m₁ and m₂ or other receptors. It is as potent as saralasin but with no agonist activity and is 10 times more potent than DuP753 in rats. It is similar in efficacy to enalapril (in those with severe hypertension) and atenolol, while more effective than losartan for mild to moderate hypertension.

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Safety

• Symbol(GHS): GHS07,GHS08,GHS09,GHS02
• Signal word: Danger
• Hazard statements: H413
• Precautionary statements: P501-P273
• Hazard Codes: Xn
• Risk Statements: 22
• Safety Statements: 26-24/25
• WGK Germany: 3
• RTECS: HM2950270
• HS Code: 29332900