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Tolvaptan
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Tolvaptan图片
CAS NO:150683-30-0
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
托伐普坦
OPC-41061
产品介绍
Tolvaptan 是一种选择性，竞争性并且具有口服活性的 vasopressin receptor 2 (V2R) 拮抗剂，抑制 AVP 诱导的血小板聚集，其IC50值为 1.28 μM。Tolvaptan 可诱导细胞凋亡，影响细胞周期。Tolvaptan 可用于低钠血症的研究。
生物活性

Tolvaptan is a selective, competitive and orally activevasopressin receptor2 (V2R) antagonist with anIC50of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia[1][2].

体外研究
(In Vitro)

Tolvaptan (0-100 μM; 24-168 h) decreases the growth of HepG2 cells[2].
Tolvaptan (20-100 μM; 24-48 h) induces cell death in HepG2 cells[2].
Tolvaptan (0-100 μM; 24-48 h) affects cell cycle of HepG2 cells[2].
Tolvaptan (0-100 μM; 24-48 h) causes DNA damage and induces apoptosis of HepG2 cells[2].
Tolvaptan (0-100 μM; 24-48 h) decreases cyclins and CDKs, and increases γ-H2AX, PARP cleavage and LC3B-II in HepG2 cells[2].
Tolvaptan (0-100 μM; 4-24 h) induces phosphorylation of JNK, ERK1/2 and p38 in HepG2 cells[2].
Tolvaptan (0-100 μM; 24-28 h) induces autophagy of HepG2 cells[2].

Cell Viability Assay[2]

Cell Line:HepG2 cells
Concentration:0-100 μM
Incubation Time:24, 48, 96 and 168 hours
Result:Time- and dose-dependently inhibited HepG2 cells with IC50s of ＞100, 52.2, 33.0 and 27.1 μM at 24, 48, 96 and 168 hours, respectively.

Cell Viability Assay[2]

Cell Line:HepG2 cells
Concentration:20, 40, 60, 80, and 100 μM
Incubation Time:24 and 48 hours
Result:Time- and dose-dependently inhibited HepG2 cell growth and caused cell death, with LDH released at a concentration over 40 μM. Caused oxidative DNA damage and increased ROS production with a concentration of 60-100 μM.

Cell Cycle Analysis[2]

Cell Line:HepG2 cells
Concentration:0-100 μM
Incubation Time:24 and 48 hours
Result:Caused cell cycle arrest at the G2 phase, dose-dependently increased the percentage of G0/G1 phase cells with a concentration of 20-60 μM and increased the percentage of G2/M phase cells with a concentration of 60-100 μM.

Western Blot Analysis[2]

Cell Line:HepG2 cells
Concentration:0-100 μM
Incubation Time:24 and 48 hours
Result:Dose-dependently decreased cyclin D1, cyclin D3, cyclin B1, CDK1, CDK2, CDK4, and CDK6, and increased γ-H2AX which is a maker of DNA double strand breaks in HepG2 cells. Increased the full length PARP into cleavage situation and induced PARP cleavage.

Apoptosis Analysis[2]

Cell Line:HepG2 cells
Concentration:0-100 μM
Incubation Time:24 and 48 hours
Result:Induced cell apoptosis with increasing caspase 3/7 activity at a dose over 40 μM.

Western Blot Analysis[2]

Cell Line:HepG2 cells
Concentration:0-100 μM
Incubation Time:4 and 24 hours
Result:Induced the activation of ERK1/2 and p38 after 4 or 24 h of exposure at a concentration over 60 μM in HepG2 cells.

Cell Autophagy Assay[2]

Cell Line:HepG2 cells
Concentration:0-100 μM
Incubation Time:24 and 48 hours
Result:Induced cell autophagy with autophagosome formation and an increasing lysosomal turnover rate.
体内研究
(In Vivo)

Tolvaptan (10 mg/kg; p.o. once per day for 22 days) improves cyclophosphamide (CP)-induced nephrotoxicity in rats[3].

Animal Model:Male albino rats with cyclophosphamide intraperitoneal injection[3]
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once per day; for 22 days
Result:Improved the level of urine volume, serum Na+, serum osmolarity, urinary creatinine, free water clearance, serum creatinine, urea, serum K+, blood pressure, urine osmolarity, fractional excretion of sodium and signs of nephrotoxicity in mice. Decreased caspase-3, Bax and pro-inflammatory cytokines, and increased antiapoptotic Bcl-2 in renal tissue of mice.
Clinical Trial
分子量

448.94

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.2275 mL11.1373 mL22.2747 mL
5 mM0.4455 mL2.2275 mL4.4549 mL
10 mM0.2227 mL1.1137 mL2.2275 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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本网站选购。