BIBS39

BIBS39 is a nonpeptide antagonist of the angiotensin II type 1 (AT1) receptor (Ki = 29 nM in rat lung membranes). It is selective for AT1 over AT2 receptors (Ki = 480 nM in isolated rat adrenal medulla), as well as alpha1-, alpha2-, beta1-, and beta2-adrenergic, adenosine A1 and A2, muscarinic M1, M2, and M3, and atrial natriuretic peptide receptors (Kis = >100 µM for all). BIBS39 (0.3-10 mg/kg) decreases diastolic blood pressure in pithed normotensive rats without affecting heart rate and in renal hypertensive rats with an increase in heart rate when administered at doses ranging from 1 to 30 mg/kg.Formal Name: 4'-[[2-butyl-6-[[(cyclohexylamino)carbonyl]amino]-1H-benzimidazol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid. CAS Number: 133085-33-3. Molecular Formula: C32H36N4O3. Formula Weight: 524.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 225, 295 nm. SMILES: CCCCC1=NC2=CC=C(NC(NC3CCCCC3)=O)C=C2N1CC4=CC=C(C5=CC=CC=C5C(O)=O)C=C4. InChi Code: InChI=1S/C32H36N4O3/c1-2-3-13-30-35-28-19-18-25(34-32(39)33-24-9-5-4-6-10-24)20-29(28)36(30)21-22-14-16-23(17-15-22)26-11-7-8-12-27(26)31(37)38/h7-8,11-12,14-20,24H,2-6,9-10,13,21H2,1H3,(H,37,38)(H2,33,34,39). InChi Key: OLQFKFSAJNUOPT-UHFFFAOYSA-N.