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

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.

CAS No. : 150683-30-0

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

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Tolvaptan:

Tolvaptan Related Antibodies

Top Publications Citing Use of Products

    Tolvaptan purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Apr 9:119679.  [Abstract]

    Tolvaptan (60 μM; 5-30 min) demonstrated that over a time gradient of 5–30 min, at a constant serum concentration of 5 %, the addition of AVPR2 antagonists significantly reduced cAMP levels in NRK-52E cells at 15, 20, and 25 min.

    Tolvaptan purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2025 Apr 9:119679.  [Abstract]

    Tolvaptan (60 μM; 6 h) in the H/R model of NRK-52E cells showed the effect of WLS-containing serum on the expression levels of senescence-related proteins by regulating the AVPR2-cAMP-PKA-CREB pathway in the H/R model of NRK-52E cells.

    Tolvaptan purchased from MedChemExpress. Usage Cited in: J Med Chem. 2024 Apr 11;67(7):5935-5944.  [Abstract]

    Tolvaptan (10 μM; 0-6 days) suppressed renal cyst formation.

    Tolvaptan purchased from MedChemExpress. Usage Cited in: J Med Chem. 2024 Apr 11;67(7):5935-5944.  [Abstract]

    Tolvaptan (1.25 mg/kg; sc; 6-12 days, daily) in ADPKD (Pkd1flox/flox; Ksp-Cre) mice showed Representative images of kidneys.

    Tolvaptan purchased from MedChemExpress. Usage Cited in: J Med Chem. 2024 Apr 11;67(7):5935-5944.  [Abstract]

    Tolvaptan (1.25 mg/kg; sc; 6-12 days, daily) in ADPKD (Pkd1flox/flox; Ksp-Cre) mice showed Hematoxylin and eosin staining of kidney sections from the indicated groups. Fractional cystic area (calculated as the cyst area divided by the total kidney area) of hematoxylin- and eosin-stained kidneys from the indicated groups.

    Tolvaptan purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2018 Nov;29(11):2658-2670.  [Abstract]

    Tolvaptan (Tol; 0.1, 0.01 nM; 30 min+6 h) failed to inhibit LCA-induced AQP2 protein expression in rat Inner medullary collecting duct cells.

    View All Vasopressin Receptor Isoform Specific Products:

    View All Isoforms
    V1a Receptor  V1b Receptor  V2 Receptor 

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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 (396 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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Tolvaptan
    Cat. No.:
    HY-17000
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (396 KB) Français - FR (396 KB) Deutsch - DE (396 KB) Norwegian - NO (396 KB) Español - ES (396 KB) Swedish - SV (396 KB) Italian - IT (396 KB) Korean - KR (396 KB) Portuguese - PT (396 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.