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Mozavaptan

Catalog No. T6288Cas No. 137975-06-5
Alias OPC31260l, OPC-31260

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

Mozavaptan

Mozavaptan

Purity: 99.12%
Catalog No. T6288Alias OPC31260l, OPC-31260Cas No. 137975-06-5
Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.
Pack SizePriceAvailabilityQuantity
10 mg$43In Stock
25 mg$68In Stock
50 mg$98In Stock
100 mg$156In Stock
1 mL x 10 mM (in DMSO)$30In Stock
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Purity:99.12%
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Product Introduction

Bioactivity
Description
Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.
Targets&IC50
V2 receptor:14 nM, Vasopressin receptor 1:1.2 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] Mozavaptan (OPC-31260) 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. 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. [2]
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[1].
AliasOPC31260l, OPC-31260
Chemical Properties
Molecular Weight427.54
FormulaC27H29N3O2
Cas No.137975-06-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 22.5 mg/mL (52.63 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3390 mL11.6948 mL23.3896 mL116.9481 mL
5 mM0.4678 mL2.3390 mL4.6779 mL23.3896 mL
10 mM0.2339 mL1.1695 mL2.3390 mL11.6948 mL
20 mM0.1169 mL0.5847 mL1.1695 mL5.8474 mL
50 mM0.0468 mL0.2339 mL0.4678 mL2.3390 mL

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