PF-05190457

PF-05190457 is an inverse agonist of the growth hormone secretagogue receptor (GHS-R), which is also known as the ghrelin receptor. It selectively binds to GHS-R (Ki = 4.37 nM) over M2 muscarinic acetylcholine receptors (mAChRs, Ki = 1,950 nM) and the serotonin (5-HT) receptor subtype 5-HT2B (IC50 = 3,700 nM). PF-05190457 (1 µM) increases glucose-induced insulin secretion in primary human pancreatic islets. It potentiates intracellular calcium levels induced by glucagon-like peptide 1 (GLP-1) in isolated dispersed rat islets when used at a concentration of 100 nM. Intragastric administration of PF-05190457 increases ex vivo vagal nerve firing rate in rats (EC50 = 10.7 nM).Formal Name: 1-[2-[(1R)-2,3-dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-ethanone. CAS Number: 1334782-79-4. Molecular Formula: C29H32N6OS. Formula Weight: 512.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Methanol: Soluble. SMILES: O=C(CC1=CN2C=C(SC2=N1)C)N3CCC4(CC3)CN(C4)[C@@H]5CCC6=CC(C7=NC=NC(C)=C7)=CC=C65. InChi Code: InChI=1S/C29H32N6OS/c1-19-11-25(31-18-30-19)22-3-5-24-21(12-22)4-6-26(24)35-16-29(17-35)7-9-33(10-8-29)27(36)13-23-15-34-14-20(2)37-28(34)32-23/h3,5,11-12,14-15,18,26H,4,6-10,13,16-17H2,1-2H3/t26-/m1/s1. InChi Key: ZIUDADZJCKGWKR-AREMUKBSSA-N.