Chemical Structure : PF-05190457
CAS No.: 1334782-79-4
Catalog No.: PC-61098Not For Human Use, Lab Use Only.
PF-05190457 (PF-5190457) is a potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.
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10 mg | $148 | In stock | |
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50 mg | $428 | In stock | |
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PF-05190457 (PF-5190457) is a potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.
PF-05190457 displays excellent off-target activity in the CEREP panel at 10 uM with exception of serotonin 5-HT2B (IC50=3.7 uM).
PF-05190457 demonstrates robust increases in glucose-stimulated insulin secretion in human islets.
M.Wt | 512.676 | |
Formula | C29H32N6OS | |
Appearance | Solid | |
Storage |
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Solubility |
DMS) >400 mM /mL (200 mg/mL) Ethanol: 200 mM/mL (103.2 mg/mL) |
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Chemical Name/SMILES |
(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 |
1. Bhattacharya SK, et al. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.
2. Kong J, et al. Br J Pharmacol. 2016 May;173(9):1452-64.
3. Denney WS, et al. Br J Clin Pharmacol. 2017 Feb;83(2):326-338.
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