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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||2.56||5 with gentle warming|
|ethanol||5.13||10 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 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||3.9 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||3.9 mL|
References are publications that support the biological activity of the product.
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 Ins secretion ex vivo. Br.J.Pharmacol. 173 1452 PMID: 26784385
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Keywords: PF 05190457, PF 05190457 supplier, PF05190457, high, affinity, selective, ghrelin, inverse, agonists, agonism, antagonists, type, II, diabetes, obesity, Ghrelin, Receptors, 6350, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.