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Submit ReviewPF 05190457
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)
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 |
| 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 Data 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 | 3.9 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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Product Datasheets for PF 05190457
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
If you know of a relevant reference for PF 05190457, please let us know.
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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
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Peptides Involved in Appetite Modulation Scientific Review
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