Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mozavaptan (OPC-31260) is a competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.
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10 mg | 在庫あり | ¥ 11,000 | |||
50 mg | 在庫あり | ¥ 34,500 | |||
100 mg | 在庫あり | ¥ 49,500 | |||
200 mg | 在庫あり | ¥ 74,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,000 |
説明 | Mozavaptan (OPC-31260) is a competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively. |
ターゲット&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] |
キナーゼ試験 | 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]. |
別名 | OPC31260l, OPC-31260 |
分子量 | 427.54 |
分子式 | C27H29N3O2 |
CAS No. | 137975-06-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (52.63 mM)
You can also refer to dose conversion for different animals. 詳細
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Mozavaptan 137975-06-5 GPCR/G Protein Vasopressin Receptor AVP OPC31260 diuretic OPC31260l hyponatremia Nonpeptide OPC-31260 SIADH OPC 31260 inhibit benzazepine arginine vasopressin-V2 Inhibitor inhibitor