High affinity and selective ghrelin receptor inverse agonist (Kd = 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.
Sold for research purposes under agreement from Pfizer Inc
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||2.56||5mM with gentle warming|
|ethanol||5.13||10mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 512.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.95 mL||9.75 mL||19.51 mL|
|5 mM||0.39 mL||1.95 mL||3.9 mL|
|10 mM||0.2 mL||0.98 mL||1.95 mL|
|50 mM||0.04 mL||0.2 mL||0.39 mL|
References are publications that support the products' biological activity.
Bhattacharya et al (2014) Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate. ACS Med.Chem.Lett. 5 474 PMID: 24900864
Kong et al (2016) 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 insulin secretion ex vivo. Br.J.Pharmacol. 173 1452 PMID: 26784385
If you know of a relevant reference for PF 05190457, please let us know.
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Keywords: PF 05190457, supplier, PF05190457, high, affinity, selective, ghrelin, inverse, agonists, agonism, antagonists, type, II, diabetes, obesity, Ghrelin, Receptors, Ghrelin, Receptors, Tocris Bioscience
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.