Tolvaptan(Synonyms: 托伐普坦; OPC-41061)

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Tolvaptan (Synonyms: 托伐普坦; OPC-41061) 纯度: 99.96%

Tolvaptan是精氨酸加压素受体2拮抗剂,能抑制AVP-诱导的血小板聚集,IC50为1.28μM。

Tolvaptan(Synonyms: 托伐普坦; OPC-41061)

Tolvaptan Chemical Structure

CAS No. : 150683-30-0

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生物活性

Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. IC50 value: 1.28 uM (inhibition of AVP-induced platelet aggregation) Target: vasopressin receptor 2 Tolvaptan (OPC-41061) is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. Tolvaptan (OPC-41061) is used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan (OPC-41061) is also in fast-track clinical trials for polycystic kidney disease. Treatment with t tolvaptan (OPC-41061) causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, tolvaptan (OPC-41061) has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, tolvaptan (OPC-41061) is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome (AHFS) to reach its primary end point for short-term efficacy without causing deleterious side effects.

Clinical Trial

分子量

448.94

Formula

C26H25ClN2O3

CAS 号

150683-30-0

中文名称

托伐普坦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (222.75 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2275 mL 11.1373 mL 22.2747 mL
5 mM 0.4455 mL 2.2275 mL 4.4549 mL
10 mM 0.2227 mL 1.1137 mL 2.2275 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (4.83 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (4.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.83 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (4.83 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Friedman B, Cirulli J. Hyponatremia in critical care patients: Frequency, outcome, characteristics, and treatment with the vasopressin V(2)-receptor antagonist tolvaptan. J Crit Care. 2012 Aug 8.

    [2]. Inomata T. Tolvaptan (vasopressin receptor antagonist).Nihon Rinsho. 2011 Nov;69 Suppl 9:408-11.

    [3]. Vaduganathan M, Gheorghiade M, Pang PS, Konstam MA, Zannad F, Swedberg K, Grinfeld L, Burnett JC Jr, Krasa HB, Zimmer C, Blair J, Ouyang J, Maggioni AP; EVEREST investigators. Efficacy of oral tolvaptan in acute heart failure patients with hypotension and renal impairment. J Cardiovasc Med (Hagerstown). 2012 Jul;13(7):415-22.

    [4]. Y Yamamura et al. OPC-41061, a Highly Potent Human Vasopressin V2-Receptor Antagonist: Pharmacological Profile and Aquaretic Effect by Single and Multiple Oral Dosing in Rats. J. Pharmacol. Exp. Ther. 1998, 287(3), 860-867.

    [5]. RW Schrier et al. Tolvaptan, a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia. N Engl J Med 2006, 355, 2099-2112.

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