Chemical Name: (R)-N-[2,3-Dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)-urea
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Beinbornet 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
Kitanoet al (2000) Long-lasting cholecystokinin2 receptor blockade after a single subcutaneous injection of YF476 or YM022. Br.J.Pharmacol. 130 699 PMID: 10821801
Nishidaet 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