SR 27897

SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist. It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 µg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 µg/kg).Formal Name: 2-[[[4-(2-chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-acetic acid. CAS Number: 136381-85-6. Synonyms: Lintitript. Molecular Formula: C20H14ClN3O3S. Formula Weight: 411.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 321 nm. SMILES: O=C(NC1=NC(C2=CC=CC=C2Cl)=CS1)C3=CC4=CC=CC=C4N3CC(O)=O. InChi Code: InChI=1S/C20H14ClN3O3S/c21-14-7-3-2-6-13(14)15-11-28-20(22-15)23-19(27)17-9-12-5-1-4-8-16(12)24(17)10-18(25)26/h1-9,11H,10H2,(H,25,26)(H,22,23,27). InChi Key: ILNRQFBVVQUOLP-UHFFFAOYSA-N.