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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 Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $43 | In Stock | |
25 mg | $68 | In Stock | |
50 mg | $98 | In Stock | |
100 mg | $156 | In Stock | |
1 mL x 10 mM (in DMSO) | $30 | In Stock |
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 | Vasopressin receptor 1:1.2 μM, V2 receptor:14 nM |
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]. |
Alias | OPC31260l, OPC-31260 |
Molecular Weight | 427.54 |
Formula | C27H29N3O2 |
Cas No. | 137975-06-5 |
Smiles | CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc12 |
Relative Density. | 1.21 g/cm3 |
Storage | Powder: -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
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