Velneperit

Velneperit is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y5 (Ki = 5.3 nM). It is selective for Y5 over Y1, Y2, and Y4 receptors, as well as a panel of 44 receptors, ion channels, transporters and enzymes, at 10 µM. Velneperit inhibits NPY-induced decreases in forskolin-induced cAMP production in CHO-K1 cells expressing the human Y5 receptor (IC50 = 169 nM). In vivo, velneperit (50 mg/kg) suppresses Y5 agonist-induced increases in food intake in high-fat diet-induced obese (DIO) mice. It also reduces body weight gain and suppresses food intake in DIO mice.Formal Name: trans-4-[[(1,1-dimethylethyl)sulfonyl]amino]-N-[5-(trifluoromethyl)-2-pyridinyl]-cyclohexanecarboxamide. CAS Number: 342577-38-2. Synonyms: S-2367. Molecular Formula: C17H24F3N3O3S. Formula Weight: 407.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 244, 279 nm. SMILES: FC(F)(F)C(C=N1)=CC=C1NC([C@H]2CC[C@@H](CC2)NS(C(C)(C)C)(=O)=O)=O. InChi Code: InChI=1S/C17H24F3N3O3S/c1-16(2,3)27(25,26)23-13-7-4-11(5-8-13)15(24)22-14-9-6-12(10-21-14)17(18,19)20/h6,9-11,13,23H,4-5,7-8H2,1-3H3,(H,21,22,24)/t11-,13-. InChi Key: WGEWUYACXPEFPO-AULYBMBSSA-N.