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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)
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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.
Blood Press. 1994 Mar;3(1-2):137-41; Br J Pharmacol. 1992 Apr;105(4):787-91.
Purity ≥98%
COA
MSDS