PF-05190457|CAS 1334782-79-4|DC Chemicals

Cas No.:	1334782-79-4
Chemical Name:	(R)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-1-(2-(5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonan-7-yl)ethan-1-one
Synonyms:	PF05190457;PF 5190457;PF5190457
SMILES:	CC1N=CN=C(C2C=C3C(=CC=2)C(N2CC4(CCN(C(=O)CC5N=C6N(C=5)C=C(C)S6)CC4)C2)CC3)C=1
Formula:	C₂₉H₃₂N₆Os
M.Wt:	512.676
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.

Description:	PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
Target:	pKi: 8.36 (Humnan ghrelin receptor)[1]
In Vivo:	PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets[1].
In Vitro:	PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity[1].
Cell Assay:	Human whole islets are incubated in assay buffer containing 2.8 mM glucose for 45 minutes at 37 °C to stabilize insulin secretion; islets are then treated with 11.2 mM glucose in the presence and absence of PF-5190457 for one hour at 37 °C. Following incubation, samples are tested for the amount of insulin secreted into the media[1].
References:	[1]. Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.

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