| CAS NO: | 137975-06-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 427.54 |
|---|---|
| Formula | C27H29N3O2 |
| 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 |
| Synonyms | OPC-31260; OPC31260l; OPC31260; OPC 31260l; OPC 31260; OPC-31260l; OPC31260 l; OPC-31260-l; OPC 31260 l |
| 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 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. |
| Animal model | Male Sprague-Dawley rats |
| Formulation & Dosage | Dissolved 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. |
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