PF 05190457

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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)
Citations (1)
Literature (1)

Biological Activity for PF 05190457

PF 05190457 is a 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Technical Data for PF 05190457

M. Wt 512.67
Formula C29H32N6OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1334782-79-4
PubChem ID 58438464
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 Data for PF 05190457

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 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.

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

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References for PF 05190457

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

1 Citation for PF 05190457

Citations are publications that use Tocris products. Selected citations for PF 05190457 include:

Chao et al (2022) Molecular mechanism of agonism and inverse agonism in ghrelin receptor. Nat Commun 13 300 PMID: 35027551

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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

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.