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Tolvaptan

Name: Tolvaptan
Brand: TargetMol
SKU: T2326
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: OPC-41061) Copy Product Info

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Synonyms: OPC-41061

Catalog No. T2326 Copy Product Info

Purity: 99.91%

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Tolvaptan (OPC-41061) is an orally active, selective, competitive vasopressin receptor 2 (V2R) antagonist (IC50 = 1.28 μM) that inhibits AVP-induced platelet aggregation. Tolvaptan is used in studies of hyponatremia.

Cas No. 150683-30-0

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Pack Size	Price	USA Stock	Global Stock
1 mg	$32	In Stock	In Stock
2 mg	$45	In Stock	In Stock
5 mg	$74	In Stock	In Stock
10 mg	$117	In Stock	In Stock
25 mg	$217	In Stock	In Stock
50 mg	$383	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$82	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.91%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Tolvaptan (OPC-41061) is an orally active, selective, competitive vasopressin receptor 2 (V2R) antagonist (IC50 = 1.28 μM) that inhibits AVP-induced platelet aggregation. Tolvaptan is used in studies of hyponatremia.
Targets & IC50	HepG2 cells:27.1 µM, V1 receptor(human):25 nM, V1 receptor(human):4.9 nM (Ki), H69 cells:53.6 μM, NTCP:31.6 μM, MRP2:> 50 μM, V2 receptor (human):1.9 nM, V2 receptor (human):0.85 nM (Ki), BSEP:∼41.5 μM, V2 receptor:3 nM
In vitro	Methods: Human renal cyst cells from ADPKD kidney donors were cultured in a 3D matrix and pretreated with 10 μM GLPG2737, 10 μM Tolvaptan, or a combination of both. Cyst formation was then induced using moxoluthine, with medication changes every 3-4 days over a total period of 11-13 days. Results: All treatment groups exhibited inhibitory effects on capsaicin-induced cyst growth. [1] Methods: HCT-8 (colon cancer), HepG2 (liver cancer), and SK-N-AS (neuroblastoma) cells were treated with 30, 50, or 70 μM Tolvaptan for 48 hours, followed by CCK-8 assay for cell viability. Results: Tolvaptan concentration-dependently inhibited cell proliferation. [2]
In vivo	Methods: Pkd1RC/RC mouse model administered treatment from 3 weeks of age to 23 weeks of age (20 weeks total). Tolvaptan administered via daily morning gavage (75 mg/kg) + evening feed (0.1% w/w) to ensure 24-hour coverage. Results: Tolvaptan monotherapy improved total kidney volume and fibrosis. [1]
Synonyms	OPC-41061
Kinase Assay	Cell-free autophosphorylation assay using time-resolved fluorometry: Neratinib is prepared as 10 mg/mL stocks in DMSO and diluted in 25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL). Purified recombinant COOH-terminal fragments of HER2 (amino acids 676-1255) or epidermal growth factor receptor (EGFR) (amino acids 645-1186) [diluted in 100 mM HEPES (pH 7.5) and 50% glycerol] is incubated with increasing concentrations of Neratinib in 4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM sodium vanadate, and 0.2 mM DTT for 15 minutes at room temperature in 96-well ELISA plates. The kinase reaction is initiated by the addition of 40 μM ATP and 20 mM MgCl2 and allowed to proceed for 1 hour at room temperature. Plates are washed, and phosphorylation is detected using Europium-labeled anti-phospho-tyrosine antibodies (15 ng/well). After washing and enhancement steps, signal is detected using a Victor2 fluorescence reader (excitation wavelength 340 nm, emission wavelength 615 nm). The concentration of Neratinib that inhibits receptor phosphorylation by 50% (IC50) is calculated from inhibition curves.

Chemical Properties

Molecular Weight	448.94
Formula	C₂₆H₂₅ClN₂O₃
Cas No.	150683-30-0
Smiles	C(=O)(N1C=2C(=CC(Cl)=CC2)C(O)CCC1)C3=C(C)C=C(NC(=O)C4=C(C)C=CC=C4)C=C3
Relative Density.	1.311 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 4.5 mg/mL (10.02 mM), Sonication is recommended.

DMSO: 240 mg/mL (534.59 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.14 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2275 mL	11.1373 mL	22.2747 mL	111.3735 mL
5 mM	0.4455 mL	2.2275 mL	4.4549 mL	22.2747 mL
10 mM	0.2227 mL	1.1137 mL	2.2275 mL	11.1373 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1114 mL	0.5569 mL	1.1137 mL	5.5687 mL
50 mM	0.0445 mL	0.2227 mL	0.4455 mL	2.2275 mL
100 mM	0.0223 mL	0.1114 mL	0.2227 mL	1.1137 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.