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Tolvaptan

Cat. No. 5181 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective vasopressin V2 receptor antagonist; renoprotective and orally active
别名： OPC-41061
化学名： N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
文献 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Tolvaptan

Tolvaptan is a potent and selective competitive vasopressin V2 receptor antagonist (Ki values are 0.06 and 12.3 nM for V2 and V1a receptors respectively). Decreases urine osmolality and increases serum sodium concentrations. Delays the onset of end-stage renal disease in a mouse model of polycystic kidney disease. Exhibits myocardial and renal protective effects in hypertensive heart failure rats. Orally active.

化合物库 for Tolvaptan

Tolvaptan is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。

技术数据 for Tolvaptan

分子量 448.94
公式 C26H25ClN2O3
储存 Store at +4°C
纯度 ≥98% (HPLC)
CAS Number 150683-30-0
PubChem ID 216237
InChI Key GYHCTFXIZSNGJT-UHFFFAOYSA-N
Smiles OC1C2=C(C=CC(Cl)=C2)N(C(C3=C(C)C=C(NC(C4=CC=CC=C4C)=O)C=C3)=O)CCC1

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 Tolvaptan

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 44.89 100

制备储备液 for Tolvaptan

以下数据基于产品分子量 448.94。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.23 mL 11.14 mL 22.27 mL
5 mM 0.45 mL 2.23 mL 4.45 mL
10 mM 0.22 mL 1.11 mL 2.23 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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产品说明书 for Tolvaptan

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Tolvaptan

参考文献是支持产品生物活性的出版物。

Kondo et al (1999) 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist. Bioorg.Med.Chem. 7 1743 PMID: 10482466

Ghali et al (2009) Tolvaptan. Nat.Rev.Drug Discov. 8 611 PMID: 19644472

Aihara et al (2014) Tolvaptan delays the onset of end-stage renal disease in a polycystic kidney disease model by suppressing increases in kidney volume and renal injury. J.Pharmacol.Exp.Ther. 349 258 PMID: 24570071

Morooka et al (2012) Chronic administration of oral vasopressin type 2 receptor antagonist tolv. exerts both myocardial and renal protective effects in rats with hypertensive heart failure. Circ.Heart.Fail. 5 484 PMID: 22628529

If you know of a relevant reference for Tolvaptan, please let us know.

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关键词: Tolvaptan, Tolvaptan supplier, Tolvaptan, potent, selective, competitive, vasopressin, receptors, antagonists, V2, renal, cardial, protective, renoprotective, hyponatremia, OPC-41061, Vasopressin, Receptors, 5181, Tocris Bioscience

1 篇 Tolvaptan 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Tolvaptan 的部分引用包括：

Zeynalov et al (2015) Arginine-Vasopressin Receptor Blocker Conivaptan Reduces Brain Edema and Blood-Brain Barrier Disruption after Experimental Stroke in Mice. Mol Cells 10 e0136121 PMID: 26275173

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