YM 022

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Cat.No. 1408 - YM 022 | C32H28N4O3 | CAS No. 145084-28-2
Description: Highly potent, selective non-peptide CCK2 antagonist
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)
Datasheet
Citations (4)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: potent selective non-peptide CCK2 antagonists Cholecystokinin2 Receptors YM022 CCK2 Receptor

4 Citations for YM 022

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

Wagner et al (2013) The dorsomedial hypothalamus mediates stress-induced hyperalgesia and is the source of the pronociceptive peptide cholecystokinin in the rostral ventromedial medulla. Neuropharmacology 238 29 PMID: 23415792

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

Karson et al (2008) Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. Br J Pharmacol 54 117 PMID: 17689570


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