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说明： Orally active vasopressin V1 antagonist
化学名： N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide
纯度： ≥98% (HPLC)
生物活性 for OPC 21268
OPC 21268 is a nonpeptide vasopressin V1 receptor antagonist. Displays greater affinity for rat V1 than human V1 (Ki values are 25 and 8800 nM respectively). Exhibits 1000-fold selectivity for V1 receptors over V2 receptors. Orally active.
化合物库 for OPC 21268
OPC 21268 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for OPC 21268
| 分子量 | 449.54 |
| 公式 | C26H31N3O4 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 131631-89-5 |
| PubChem ID | 114904 |
| InChI Key | KSNUCNRMDYJBKT-UHFFFAOYSA-N |
| Smiles | O=C2N(C3CCN(C(C4=CC=C(OCCCNC(C)=O)C=C4)=O)CC3)C1=CC=CC=C1CC2 |
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 OPC 21268
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.95 | 100 | |
| ethanol | 11.24 | 25 |
制备储备液 for OPC 21268
以下数据基于产品分子量 449.54。 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 | 2.22 mL | 11.12 mL | 22.24 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.45 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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产品说明书 for OPC 21268
参考文献 for OPC 21268
参考文献是支持产品生物活性的出版物。
Yamamura et al (1991) OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science 252 572 PMID: 1850553
Imaizumi et al (1992) Effects of OPC-21268, an orally effective vasopressin V1 receptor antagonist in humans. Hypertension 20 54 PMID: 1319959
Thibonnier et al (2000) A molecular model of agonist and nonpeptide antagonist binding to the human V1 vascular vasopressin receptor. J.Pharmacol.Exp.Ther. 294 195 PMID: 10871312
If you know of a relevant reference for OPC 21268, please let us know.
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关键词: OPC 21268, OPC 21268 supplier, OPC21268, vasopressin, v1, v1r, avp, arginine, Vasopressin, Receptors, 3924, Tocris Bioscience
3 篇 OPC 21268 的引用文献
引用文献是使用了 Tocris 产品的出版物。 OPC 21268 的部分引用包括：
Amita et al (2018) Asymmetric vasopressin signaling spatially organizes the master circadian clock. J Comp Neurol 526 2048-2067 PMID: 29931690
Gallia et al (2022) Evidence for a Prehypertensive Water Dysregulation Affecting the Development of Hypertension: Results of Very Early Treatment of Vasopressin V1 and V2 Antagonism in Spontaneously Hypertensive Rats. Front Cardiovasc Med 9 897244 PMID: 35722114
Harshida et al (2020) Reduced VIP Expression Affects Circadian Clock Function in VIP-IRES-CRE Mice (JAX 010908). J Biol Rhythms 35 340-352 PMID: 32460660
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.