YM 022

Cat. No. 1408

YM 022 C32H28N4O3 [145084-28-2]

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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

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
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>99 %
Storage:
Store at RT
CAS No:
145084-28-2

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

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.

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.

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 and in vivo. J.Pharmacol.Exp.Ther. 269 725. PMID: 7910212.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for YM 022 include:

Saia et al (2014) Cholecystokinin inhibits inducible nitric oxide synthase expression by lipopolysaccharide-stimulated peritoneal macrophages. Mediators Inflamm 2014 896029. PMID: 25125801.

Marshall et al (2012) Activation of descending pain-facilitatory pathways from the rostral ventromedial medulla by cholecystokinin elicits release of prostaglandin-E2 in the spinal cord. Pain 153 86. PMID: 22030324.

Do you know of a great paper that uses YM 022 from Tocris? If so please let us know.

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Keywords: YM 022, supplier, potent, selective, non-peptide, CCK2, antagonists, Cholecystokinin2, Receptors, YM022, Tocris Bioscience, CCK2 Receptor Antagonist products

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