PF 05190457

Key Product Details

Product Description

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

Product Specifications for PF 05190457

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

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 4 publications citing the usage of this 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

Product Documents for PF 05190457