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PF-05190457

Chemical Structure : PF-05190457

CAS No.: 1334782-79-4

PF-05190457 (PF05190457;PF 5190457;PF5190457)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 512.676
Formula C29H32N6OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMS) >400 mM /mL (200 mg/mL) Ethanol: 200 mM/mL (103.2 mg/mL)

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

References

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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