Mozavaptan (OPC-31260)

Alias: Mozavaptan; OPC-31260; OPC31260l; OPC31260; OPC 31260l; OPC 31260; OPC-31260l; OPC31260 l; OPC-31260-l; OPC 31260 l

Cat No.:V1486 Purity: ≥98%

COA Product Data Instructions for use SDS

Mozavaptan (OPC-31260) Chemical Structure CAS No.: 137975-06-5
Product category: Vasopressin Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Mozavaptan (OPC-31260):

Mozavaptan HCl (OPC 31260)

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators

Product Description

Mozavaptan (formerly known as OPC-31260; OPC-31260l; OPC31260; OPC31260l) is an orally bioactive, selective and competitive vasopressin receptor antagonist for both V1 and V2 receptors with anti-hypernatremic activity. It inhibits the vasopressin V1 and V2 receptors with IC50s of 1.2 μM and 14 nM, respectively. Otsuka Pharm created and distributed mozavaptan in Japan. October 2006 saw the approval of mozavaptan in Japan for the treatment of hyponatremia, or low blood sodium levels, brought on by tumors that produce too much ADH and cause syndrome of inappropriate antidiuretic hormone (SIADH).

Biological Activity I Assay Protocols (From Reference)

Targets

Vasopressin V2 receptor ( IC50 = 14 nM ); Vasopressin V1 receptor ( IC50 = 1.2 μM )

ln Vitro

In vitro activity: Mozavaptan (OPC-31260) is approximately 100 times more selective for V2 receptors and inhibits AVP binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner. Rat kidney has a [3H]-AVP K_d value of 1.38 nM, whereas rat liver has a value of 1.1 nM. In rat liver and kidney, mozavaptan significantly lowers the [3H]-AVP K_d (K_d of 2.47 nM and 5.51 nM for V1 receptor at 0.3 μM and 1 μM, respectively; K_d of 2.4 nM and 4.03 nM for V2 receptor at 0.3 μM and 1 μM, respectively)[1].

ln Vivo

Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment increases urine flow and lowers urine osmolality in a dose-dependent manner[1].
Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment dose-dependently blocks the antidiuretic effect of exogenously administered arginine vasopressin (AVP) in rats anesthetized with alcohol and loaded with water[1].

Enzyme Assay

To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasing concentrations of [3H]-AVP with or without excess (1 μM) unlabelled AVP to obtain a saturation curve. Mozavaptan interacts either noncompetitively or competitively, as determined by examining the saturation binding of [3H]-AVP in liver membranes at concentrations of 0.3 μM and 1 μM, and in kidney membranes at concentrations of 3 nM and 10 nM. The Scatchard method is used to plot the data on the saturation curve, and regression analysis is used to fit the data.

Animal Protocol

Dissolved in 3% ethanol (v/v), 1.67% glucose (w/v) and 0.3% NaCl (w/v); 10, 30, 100μg/kg; i.v. injection

Male Sprague-Dawley rats

References

[1]. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.

[2]. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C27H29N3O2

Molecular Weight

427.54

Exact Mass

427.23

Elemental Analysis

C, 75.85; H, 6.84; N, 9.83; O, 7.48

CAS #

137975-06-5

Related CAS #

Mozavaptan hydrochloride; 138470-70-9

Appearance

Solid powder

SMILES

CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C

InChi Key

WRNXUQJJCIZICJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C27H29N3O2/c1-19-9-4-5-10-22(19)26(31)28-21-16-14-20(15-17-21)27(32)30-18-8-13-24(29(2)3)23-11-6-7-12-25(23)30/h4-7,9-12,14-17,24H,8,13,18H2,1-3H3,(H,28,31)

Chemical Name

N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide

Synonyms

Mozavaptan; OPC-31260; OPC31260l; OPC31260; OPC 31260l; OPC 31260; OPC-31260l; OPC31260 l; OPC-31260-l; OPC 31260 l

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 1~85 mg/mL (2.3~198.8 mM)

Water: <1 mg/mL

Ethanol: ~1 mg/mL (~2.3 mM)

Solubility (In Vivo)

30%Propylene glycol, 5%Tween 80, 65% D5W: 30 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3390 mL	11.6948 mL	23.3896 mL
	5 mM	0.4678 mL	2.3390 mL	4.6779 mL
	10 mM	0.2339 mL	1.1695 mL	2.3390 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.