Cat. No.: HY-17000

Tolvaptan

(Synonyms: OPC-41061)

19 Cited Publications

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Based on 19 publication(s) in Google Scholar

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.

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Pureté: 99.95%
CAS No.: 150683-30-0
Formule: C₂₆H₂₅ClN₂O₃
Masse moléculaire:448.94

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tolvaptan Chemical Structure

CAS No.: 150683-30-0

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (19)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target

V2 Receptor

Voir tous les produits spécifiques à Isoform Vasopressin 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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 150683-30-0
Appearance Solid
Masse moléculaire 448.94
Formule C₂₆H₂₅ClN₂O₃
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
Synonyms

OPC-41061
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (19)

All In Vivo ImagingELISAHistological Imaging/StainingWB

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Journal Impact Factor

Nat Commun

Structural insights into antagonist recognition by the vasopressin V2 receptor. [Abstract]

2025 Nov 4;16(1):9734. PMID: 41188237
J Am Soc Nephrol

Bile Acid G Protein-Coupled Membrane Receptor TGR5 Modulates Aquaporin 2-Mediated Water Homeostasis. [Abstract]

2018 Nov;29(11):2658-2670. PMID: 30305310

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.
J Med Chem

Long-Residence Time Peptide Antagonist for the Vasopressin V2 Receptor to Treat Autosomal Dominant Polycystic Kidney Disease. [Abstract]

2024 Apr 11;67(7):5935-5944. PMID: 38509003

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 (Pkd1^flox/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 (Pkd1^flox/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.
J Med Chem

Benzodiazepine Derivatives as Potent Vasopressin V2 Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease. [Abstract]

2022 Jul 14;65(13):9295-9311. PMID: 35579344
Int J Nanomedicine

Tolvaptan-Loaded Tomato-Derived Nanovesicles: Characterization and Evaluation of Cytotoxicity, Wound Healing Potential and the Effects on Cyst Formation in Renal Cell Lines. [Abstract]

2025 May 17:20:6253-6269. PMID: 40400781
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
J Ethnopharmacol

Wuling San regulates AVPR2-cAMP-PKA-CREB pathway to delay cellular senescence and ameliorate acute kidney injury. [Abstract]

2025 Apr 9:119679. PMID: 40216046

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.
J Mol Liq

2024 Nov 15.
Int J Mol Sci

A Role for Both V1a and V2 Receptors in Renal Heat Stress Injury Amplified by Rehydration with Fructose. [Abstract]

2019 Nov 16;20(22):5764. PMID: 31744099
Eur J Pharmacol

Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective. [Abstract]

2020 Aug 5;880:173157. PMID: 32360346
Drug Dev Res

Desmopressin Induces Mitochondrial Fragmentation and Dysfunction in Human U87 MG Glioma Cells via CaMKII-Drp1 Signaling Pathway. [Abstract]

2026 Feb;87(1):e70224. PMID: 41527347
FASEB J

Hydrogen sulfide upregulates renal AQP-2 protein expression and promotes urine concentration. [Abstract]

2019 Jan;33(1):469-483. PMID: 30036087
Sci Rep

Characterization of five novel vasopressin V2 receptor mutants causing nephrogenic diabetes insipidus reveals a role of tolvaptan for M272R-V2R mutation. [Abstract]

2020 Oct 2;10(1):16383. PMID: 33009446
Am J Physiol Renal Physiol

Aliskiren increases aquaporin-2 expression and attenuates lithium-induced nephrogenic diabetes insipidus. [Abstract]

2017 Oct 1;313(4):F914-F925. PMID: 28228402
J Pharm Biomed Anal

2025 Jun.
Neurogastroenterol Motil

Vasopressin augments TNBS-induced colitis through enteric neuronal V1a receptor-mediated COX-2-dependent prostaglandin release from mast cells in mice. [Abstract]

2019 Feb;31(2):e13493. PMID: 30334342
Biochem Biophys Res Commun

Arginine vasopressin and angiotensin II coregulate Aquaporin 2 expression in M-1 cells. [Abstract]

2025 Jan:745:151256. PMID: 39740402
Nat Prod Commun

2025 Jan 29.
SSRN

2023 May 30.

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (289 KB)
SDS (396 KB)
- 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)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wu Y, et al. Mechanisms of tolvaptan-induced toxicity in HepG2 cells. Biochem Pharmacol. 2015 Jun 15;95(4):324-36. [Content Brief]

[2]. El-Shabrawy M, et al. Protective effect of tolvaptan against cyclophosphamide-induced nephrotoxicity in rat models. Pharmacol Res Perspect. 2020 Oct;8(5):e00659. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Tolvaptan

19 Cited Publications

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Tolvaptan

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Publications Citing Use of MedChemExpress (MCE) Tolvaptan

Voir tous les produits spécifiques à Isoform Vasopressin Receptor

Activité biologique

Chemical Information

Publications (19)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tolvaptan Related Classifications

Cat. No.: HY-17000