SSR 240612

SSR 240612 is a selective, non-peptide antagonist of the bradykinin B1 receptor (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively). It inhibits the contraction of rabbit aorta and rat ileum induced by the B1 receptor agonist des-Arg9-bradykinin (des-Arg9-BK) ex vivo in a concentration-dependent manner. SSR 240612 (0.3 mg/kg) reduces tissue damage and neutrophil accumulation in a rat model of splanchnic artery occlusion/reperfusion-induced intestinal injury and inhibits des-Arg9-BK-induced paw edema in mice when administered orally at doses of 3 and 10 mg/kg or intraperitoneally at doses of 0.3 and 1 mg/kg. SSR 240612 (10 mg/kg per day) reduces fibrosis in a unilateral ureteral obstruction mouse model of kidney fibrosis. It also reduces mean arterial blood pressure in two rat models of hypertension when administered at doses of 5 and 10 mg/kg and reduces plasma glucose and insulin levels in a glucose-fed rat model of insulin resistance when administered at a dose of 10 mg/kg per day. SSR 240612 also exhibits analgesic properties in several rodent models of hyperalgesia.Formal Name: (3R)-3-(1,3-benzodioxol-5-yl)-N-[(6-methoxy-2-naphthalenyl)sulfonyl]-beta-alanyl-4-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]methyl]-N-methyl-N-(1-methylethyl)-D-phenylalaninamide, monohydrochloride. CAS Number: 464930-42-5. Molecular Formula: C42H52N4O7S . HCl. Formula Weight: 793.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 241, 286 nm. SMILES: C[C@@H]1N(CC2=CC=C(C[C@H](C(N(C)C(C)C)=O)NC(C[C@H](C3=CC=C(OCO4)C4=C3)NS(C5=CC(C=CC(OC)=C6)=C6C=C5)(=O)=O)=O)C=C2)[C@H](C)CCC1.Cl. InChi Code: InChI=1S/C42H52N4O7S.ClH/c1-27(2)45(5)42(48)38(20-30-10-12-31(13-11-30)25-46-28(3)8-7-9-29(46)4)43-41(47)24-37(34-16-19-39-40(23-34)53-26-52-39)44-54(49,50)36-18-15-32-21-35(51-6)17-14-33(32)22-36,/h10-19,21-23,27-29,37-38,44H,7-9,20,24-26H2,1-6H3,(H,43,47),1H/t28-,29+,37-,38-,/m1./s1. InChi Key: GLHHFOSVBQQNAW-GDYXXZBVSA-N.