PF 05190457

Name: PF 05190457
Brand: Tocris Bioscience
SKU: 6350

Tocris Bioscience, part of Bio-Techne | Catalog # 6350

Citations (3)

COA / SDS

High affinity and selective ghrelin receptor inverse agonist

Key Product Details

Description:	High affinity and selective ghrelin receptor inverse agonist
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
Purity:	≥98% (HPLC)
Molecular Weight:	512.67

View Full Technical Details for PF 05190457

Technical Data
Citations

Biological Activity for PF 05190457

PF 05190457 is a high affinity and selective ghrelin receptor inverse agonist (K_d = 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Technical Data for PF 05190457

M. Wt	512.67
Formula	C₂₉H₃₂N₆O_S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1334782-79-4
PubChem ID	58438464
InChi Key	ZIUDADZJCKGWKR-AREMUKBSSA-N
Smiles	CC1=CC(C2=CC(CC[C@H]3N4CC5(CCN(C(CC6=CN7C(SC(C)=C7)=N6)=O)CC5)C4)=C3C=C2)=NC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 05190457

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	2.56	5 with gentle warming
	ethanol	5.13	10 with gentle warming

Preparing Stock Solutions for PF 05190457

The following data is based on the product molecular weight 512.67.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	19.51 mL	97.53 mL	195.06 mL
0.5 mM	3.90 mL	19.51 mL	39.01 mL
1 mM	1.95 mL	9.75 mL	19.51 mL
5 mM	0.39 mL	1.95 mL	3.90 mL

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References for PF 05190457

References are publications that support the biological activity of the product.

Kong 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. Br.J.Pharmacol. 2016 PMID: 26784385
Bhattacharya Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate. ACS Med.Chem.Lett. 2014 PMID: 24900864