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

Tolvaptan  (Synonyms: OPC-41061)

Cat. No.: HY-17000 Purity: 99.95%
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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.

For research use only. We do not sell to patients.

Tolvaptan Chemical Structure

Tolvaptan Chemical Structure

CAS No. : 150683-30-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 158 In-stock
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Solid
5 mg USD 92 In-stock
10 mg USD 144 In-stock
50 mg USD 465 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Tolvaptan:

Tolvaptan Related Antibodies

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V1a Receptor  V1b Receptor  V2 Receptor 

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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].

IC50 & Target

V2 Receptor 

 

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].

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

Tolvaptan Related Antibodies

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.
In Vivo

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

MedChemExpress (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
Molecular Weight

448.94

Formula

C26H25ClN2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC=C1C)NC2=CC=C(C(C)=C2)C(N3CCCC(C4=CC(Cl)=CC=C43)O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (222.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

SDS (393 KB)

COA (257 KB) RP-HPLC (251 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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
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Tolvaptan Related Classifications

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.

Keywords:

Tolvaptan150683-30-0OPC-41061OPC41061OPC 41061Vasopressin ReceptorAutophagyhyponatremiaantidiuretic hormoneSIADHcell cycleapoposisInhibitorinhibitorinhibit

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