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说明： Highly potent, selective non-peptide CCK2 antagonist
化学名： (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
纯度： ≥99% (HPLC)
生物活性 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.
技术数据 for YM 022
| 分子量 | 516.6 |
| 公式 | C32H28N4O3 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for YM 022
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 51.66 | 100 | |
| ethanol | 5.17 | 10 |
制备储备液 for YM 022
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for YM 022
参考文献 for YM 022
参考文献是支持产品生物活性的出版物。
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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关键词: YM 022, YM 022 supplier, potent, selective, non-peptide, CCK2, antagonists, Cholecystokinin2, Receptors, YM022, Receptor, 1408, Tocris Bioscience
4 篇 YM 022 的引用文献
引用文献是使用了 Tocris 产品的出版物。 YM 022 的部分引用包括：
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.