VU0453379 (hydrochloride)

VU0453379 is an allosteric agonist and positive allosteric modulator (ago-PAM) of glucagon-like peptide 1 receptor (GLP-1R). It induces calcium mobilization in 9-3-H cells expressing human GLP-1R (EC50 = 1.3 µM) and enhances GLP-1-, exenatide-, or liraglutide-induced calcium mobilization in the same cells (EC50s = 1.8, 8.4, and 30 µM, respectively). VU0453379 (30 µM) potentiates exenatide-induced insulin secretion in primary mouse pancreatic islets. It reverses catalepsy induced by haloperidol (Cay-12014) in a rat model of Parkinson's disease motor symptoms when administered at a dose of 30 mg/kg.Formal Name: 2-cyclopentyl-2,9-dihydro-9-methyl-N-[[(2S)-1-(1-methylethyl)-2-pyrrolidinyl]methyl]-1-oxo-1H-pyrido[3,4-b]indole-4-carboxamide, monohydrochloride. Molecular Formula: C26H34N4O2 . HCl. Formula Weight: 471.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: O=C(C(C(C1=CC=CC=C12)=C3N2C)=CN(C4CCCC4)C3=O)NC[C@@H]5CCCN5C(C)C.Cl. InChi Code: InChI=1S/C26H34N4O2.ClH/c1-17(2)29-14-8-11-19(29)15-27-25(31)21-16-30(18-9-4-5-10-18)26(32)24-23(21)20-12-6-7-13-22(20)28(24)3,/h6-7,12-13,16-19H,4-5,8-11,14-15H2,1-3H3,(H,27,31),1H/t19-,/m0./s1. InChi Key: OCMGNMGYQPPMFF-FYZYNONXSA-N.