Tolvaptan

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Chemical Structure| 150683-30-0 同义名 : OPC-41061
CAS号 : 150683-30-0
货号 : A207823
分子式 : C26H25ClN2O3
纯度 : 97%
分子量 : 448.94
MDL号 : MFCD09838782
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(233.88 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Vasopressin receptor 2

    vasopressin receptor 2, IC50:3 nM
描述 Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01348035 - Completed - Japan ... 展开 >> Department of Urology, Kyorin University Hospital Mitaka, Tokyo, Japan, 181-8611 收起 <<
NCT02084797 Electrolyte Imbalance ... 展开 >> Hyponatremia Hypernatremia 收起 << Not Applicable Completed - United States, Michigan ... 展开 >> Oakland University Rochester, Michigan, United States, 48309 收起 <<
NCT02994394 Healthy Adult Male Phase 1 Completed - Japan ... 展开 >> Kyusyu region, Japan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.14mL

2.23mL

1.11mL

22.27mL

4.45mL

2.23mL
参考文献

[1]Reif GA, Yamaguchi T, et al. Tolvaptan inhibits ERK-dependent cell proliferation, Cl⁻ secretion, and in vitro cyst growth of human ADPKD cells stimulated by vasopressin. Am J Physiol Renal Physiol. 2011 Nov;301(5):F1005-13.

[2]Miyazaki T, Fujiki H, et al. Tolvaptan, an orally active vasopressin V(2)-receptor antagonist - pharmacology and clinical trials. Cardiovasc Drug Rev. 2007 Spring;25(1):1-13.