PF 05190457
Tocris Bioscience, part of Bio-Techne | Catalog # 6350
High affinity and selective ghrelin receptor inverse agonist
Key Product Details
Description
High affinity and selective ghrelin receptor inverse agonist
Product Description
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 IncProduct Specifications
Molecular Weight
512.67
Formula
C29H32N6OS
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 | 3.90 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 | 3.90 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Kong 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. 2016 PMID: 26784385
- Bhattacharya Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate. ACS Med.Chem.Lett. 2014 PMID: 24900864
Product Specific Notices for PF 05190457
For research use only
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