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    Mozavaptan (OPC-31260)
    Mozavaptan (OPC-31260)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1486
    CAS #: 137975-06-5Purity ≥98%

    Description: Mozavaptan, also known as OPC 31260 and OPC31260l,  is a orally active, selective and competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively. It was developed and marketed by Otsuka of Japan. Mozavaptan was approved in October 2006 in Japan for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors. 

    References: Blood Press. 1994 Mar;3(1-2):137-41; Br J Pharmacol. 1992 Apr;105(4):787-91. 

    Related CAS #: 138470-70-9 (HCl)   137975-06-5 (free base)   

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    Molecular Weight (MW)427.54
    FormulaC27H29N3O2 
    CAS No.137975-06-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 1 mg/mL (2.3 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  
    SynonymsOPC-31260; OPC31260; OPC 31260; OPC31260l; OPC 31260l; OPC-31260l; OPC31260 l; OPC-31260-l; OPC 31260 l


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    In Vitro

    In vitro activity: 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. Mozavaptan (OPC-31260) inhibits AVP binding to V1 and V2 receptors in a competitive manner.


    Kinase 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. To investigate whether mozavaptan interacts competitively or noncompetitively, the saturation binding of [3H]-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 μM and 1 μM in liver membranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted according to the method of Scatchard and fitted by a regression analysis.

    In VivoMozavaptan (OPC-31260) inhibits the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. OPC-31260 dose-dependently increases urine flow and decreased urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats.
    Animal modelMale Sprague-Dawley rats 
    Formulation & DosageDissolved in 3% ethanol (v/v), 1.67% glucose (w/v) and 0.3% NaCl (w/v); 10, 30, 100μg/kg; i.v. injection
    References

    Blood Press. 1994 Mar;3(1-2):137-41; Br J Pharmacol. 1992 Apr;105(4):787-91. 


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

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