1. GPCR/G Protein Autophagy
  2. Vasopressin Receptor Autophagy
  3. Tolvaptan

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

目录号: HY-17000 纯度: 99.96%
COA 产品使用指南

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。

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Tolvaptan Chemical Structure

Tolvaptan Chemical Structure

CAS No. : 150683-30-0

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10 mM * 1 mL in DMSO ¥1188
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5 mg ¥675
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10 mg ¥1080
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50 mg ¥3464
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C26H25ClN2O3

CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (222.75 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.17 mg/mL (4.83 mM); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    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。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.96%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2275 mL 11.1373 mL 22.2747 mL 55.6867 mL
5 mM 0.4455 mL 2.2275 mL 4.4549 mL 11.1373 mL
10 mM 0.2227 mL 1.1137 mL 2.2275 mL 5.5687 mL
15 mM 0.1485 mL 0.7425 mL 1.4850 mL 3.7124 mL
20 mM 0.1114 mL 0.5569 mL 1.1137 mL 2.7843 mL
25 mM 0.0891 mL 0.4455 mL 0.8910 mL 2.2275 mL
30 mM 0.0742 mL 0.3712 mL 0.7425 mL 1.8562 mL
40 mM 0.0557 mL 0.2784 mL 0.5569 mL 1.3922 mL
50 mM 0.0445 mL 0.2227 mL 0.4455 mL 1.1137 mL
60 mM 0.0371 mL 0.1856 mL 0.3712 mL 0.9281 mL
80 mM 0.0278 mL 0.1392 mL 0.2784 mL 0.6961 mL
100 mM 0.0223 mL 0.1114 mL 0.2227 mL 0.5569 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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