Formulation: A solid
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
Purity: ≥95%
Formula Markup: C29H32N6OS
Formula Weight: 512,7
Shelf life (days): 1460
CAS Number: 1334782-79-4
Notes: PF-05190457 is an inverse agonist of the growth hormone secretagogue receptor (GHS-R), which is also known as the ghrelin receptor.{51642} 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.{51643} Intragastric administration of PF-05190457 increases ex vivo vagal nerve firing rate in rats (EC50 = 10.7 nM).
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