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Mozavaptan Vasopressin Receptor antagonist

Name: Mozavaptan
Brand: Selleck Chemicals
SKU: S2920
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S2920

Mozavaptan (OPC-31260) is a novel competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.

Chemical Structure

Molecular Weight: 427.54

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras GPR GluR Prostaglandin Receptor CXCR Adenosine Receptor P2 Receptor CCR Angiotensin Receptor Hedgehog/Smoothened S1P Receptor PKA Cannabinoid Receptor cAMP Glucagon Receptor SGLT Opioid Receptor Sigma Receptor PAR Endothelin Receptor LTR Neurokinin Receptor Guanylate Cyclase PKG LPA Receptor
Related Products	RO 5028442 (RG7713) Lixivaptan (VPA-985) Mozavaptan (hydrochloride)

Chemical Information, Storage & Stability

Molecular Weight	427.54	Formula	C₂₇H₂₉N₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	137975-06-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	OPC-31260			Smiles	CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (198.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (70.17mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Vasopressin receptor 2 ^[2] 14 nM Vasopressin receptor 1 ^[2] 1.2 μM
In vitro	Mozavaptan (OPC-31260) is a nonpeptide, orally effective competitive inhibitor of AVP with a V2:V1 receptor selectivity ratio of 25:1 indicating relative V2 receptor selectivity. ^[1] This compound inhibits AVP binding to V1 and V2 receptors in a competitive manner. ^[2]
In vivo	Mozavaptan (OPC-31260) inhibits the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. This compound dose-dependently increases urine flow and decreased urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/8199714/ [2] https://pubmed.ncbi.nlm.nih.gov/1387020/

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