Chemical 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
Biological ActivityPF 05190457 is a high affinity and selective ghrelin receptor inverse agonist (Kd = 3 nM). Exhibits selectivity for ghrelin receptors over a panel of other targets. Increases intracellular Ca2+ concentration in and insulin secretion from human islets in vitro. Increases gastric afferent nerve activity in a rat ex vivo stomach preparation.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate.
Bhattacharya et al.
ACS Med.Chem.Lett., 2014;5:474
Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent Ins secretion ex vivo.
Kong et al.
Citation for PF 05190457
The citations listed below are publications that use Tocris products. Selected citations for PF 05190457 include:
1 Citation: Showing 1 - 1
Molecular mechanism of agonism and inverse agonism in ghrelin receptor.
Authors: Chao Et al.
Nat Commun 2022;13:300
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