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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)
Biological Activity for YM 022
YM 022 is an 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 for YM 022
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for YM 022
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.66 | 100 | |
| ethanol | 5.17 | 10 |
Preparing Stock Solutions for YM 022
The following data is based on the product molecular weight 516.6. Batch specific molecular weights may vary from batch to batch due to the degree 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 for YM 022
References for YM 022
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for YM 022, please let us know.
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Keywords: YM 022, YM 022 supplier, potent, selective, non-peptide, CCK2, antagonists, Cholecystokinin2, Receptors, YM022, Receptor, 1408, Tocris Bioscience
4 Citations for YM 022
Citations are publications that use Tocris products. Selected citations for YM 022 include:
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
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
Karson et al (2008) Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. Br J Pharmacol 54 117 PMID: 17689570
Do you know of a great paper that uses YM 022 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.