Biological Activity
Extremely potent and highly selective non-peptide CCK2 silent antagonist (Ki values are 68 pM and 63 nM at CCK2 and CCK1 receptors respectively). Acts in vivo to potently inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation with a long duration of action.
Technical Data
| M. Wt | 516.6 |
| Formula | C32H28N4O3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 145084-28-2 |
| PubChem ID | 3452843 |
| InChI Key | YCXFHPUBGMMWJQ-UHFFFAOYSA-N |
| Smiles | CC1=CC(NC(=O)NC2N=C(C3=CC=CC=C3)C3=CC=CC=C3N(CC(=O)C3=C(C)C=CC=C3)C2=O)=CC=C1 |
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 | 51.66 | 100 | |
| ethanol | 5.17 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 516.6. 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 | 1.94 mL | 9.68 mL | 19.36 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.87 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Beinborn et al (1998) Small synthetic ligands of the cholecystokinin-B/gastrin receptor can mimic the function of endogenous peptide hormones. Yale J.Biol.Med. 71 337 PMID: 10461364
Kitano et al (2000) Long-lasting cholecystokinin2 receptor blockade after a single subcutaneous injection of YF476 or YM022. Br.J.Pharmacol. 130 699 PMID: 10821801
Nishida et al (1994) Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro J.Pharmacol.Exp.Ther. 269 725 PMID: 7910212
Keywords: YM 022, supplier, potent, selective, non-peptide, CCK2, antagonists, Cholecystokinin2, Receptors, YM022, CCK2, Receptor, CCK2, Receptor, Tocris Bioscience
