PF 05190457

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Cat.No. 6350 - PF 05190457 | C29H32N6OS | CAS No. 1334782-79-4
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)
Datasheet
Citations
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Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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

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Product Datasheets

Safety Datasheet

References

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


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