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说明： Potent and selective vasopressin V1B antagonist
别名： Nelivaptan
化学名： (2S,4R)-1-[(3R)-5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-(2-methoxyphenyl)-2-oxo-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for SSR 149415
SSR 149415 is a potent and selective vasopressin V1B antagonist (Ki values are 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Displays >70-fold selectively for rat V1B over V1A, V2 oxytoxin and a range of other receptors and ion channels. Inhibits AVP-induced glucagon release in In-R1-G9 α-pancreatic cells in vitro. Inhibits stress-induced ACTH release and exhibits anxiolytic-like effects in anxiety models. Orally bioavailable.
化合物库 for SSR 149415
SSR 149415 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 SSR 149415
| 分子量 | 630.11 |
| 公式 | C30H32ClN3O8S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 439687-69-1 |
| PubChem ID | 9895468 |
| InChI Key | NJXZWIIMWNEOGJ-WEWKHQNJSA-N |
| Smiles | COC1=CC(OC)=C(S(=O)(N2C([C@@](C3=CC(Cl)=CC=C23)(C4=C(C=CC=C4)OC)N5C[C@@H](C[C@H]5C(N(C)C)=O)O)=O)=O)C=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 SSR 149415
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 63.01 | 100 | |
| ethanol | 63.01 | 100 |
制备储备液 for SSR 149415
以下数据基于产品分子量 630.11。 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 | 1.59 mL | 7.94 mL | 15.87 mL |
| 5 mM | 0.32 mL | 1.59 mL | 3.17 mL |
| 10 mM | 0.16 mL | 0.79 mL | 1.59 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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产品说明书 for SSR 149415
参考文献 for SSR 149415
参考文献是支持产品生物活性的出版物。
Serradeil-Le Gal et al (2005) An overview of SSR149415, a selective nonpeptide vasopressin V1b receptor antagonist for the treatment of stress-related disorders. CNS Drug Rev. 11 53 PMID: 15867952
If you know of a relevant reference for SSR 149415, please let us know.
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关键词: SSR 149415, SSR 149415 supplier, SSR149415, vasopressin, receptor, V1b, potent, selective, antagonists, antagonism, orally, bioavailable, Nelivaptan, Vasopressin, Receptors, 6195, Tocris Bioscience
2 篇 SSR 149415 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SSR 149415 的部分引用包括：
Mengliang et al (2021) Left-right side-specific endocrine signaling complements neural pathways to mediate acute asymmetric effects of brain injury. Elife 10 PMID: 34372969
Pung-Pung et al (2020) Arginine Vasopressin Modulates Ion and Acid/Base Balance by Regulating Cell Numbers of Sodium Chloride Cotransporter and H+-ATPase Rich Ionocytes. Int J Mol Sci 21 PMID: 32486459
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该领域的文献
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。
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.