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Product IntroductionBioactivity英文名: Mozavaptan描述: Mozavaptan (OPC-31260) 是 benzazepine 衍生物，是一种竞争性加压素受体拮抗剂，作用于 V1 和 V2 受体，
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Product Introduction
Bioactivity
英文名: Mozavaptan
描述: Mozavaptan (OPC-31260) 是 benzazepine 衍生物，是一种竞争性加压素受体拮抗剂，作用于 V1 和 V2 受体，IC50 分别为 1.2 μM 和 14 nM。它可在体内拮抗精氨酸加压素的抗利尿作用，可用于低钠血症、抗利尿激素不适当综合征和充血性心力衰竭的研究。
激酶实验: 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].
体外活性: Mozavaptan (OPC-31260) 是一种非肽类、口服有效的竞争性抗利尿激素(AVP)抑制剂，具有25:1的V2至V1受体选择性比率，表明其相对于V2受体的选择性。[1] Mozavaptan (OPC-31260) 竞争性抑制AVP与V1和V2受体的结合。[2]
体内活性: Mozavaptan (OPC-31260) 在水负荷、醉酒麻醉的大鼠中，以剂量依赖的方式抑制了外源性AVP的抗利尿作用。在常规清醒大鼠中，经口给予1至30 mg/kg剂量的OPC-31260，能剂量依赖性地增加尿流并降低尿渗透压。[2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 22.5 mg/mL (52.63 mM)
关键字: AVP | OPC31260 | diuretic | Mozavaptan | hyponatremia | Nonpeptide | SIADH | OPC 31260 | inhibit | benzazepine | Vasopressin Receptor | arginine | vasopressin-V2 | Inhibitor
相关产品: OPC-51803 | Conopressin S acetate(111317-90-9 free base) | RG7713 | Val9-Oxytocin | Atosiban | Desmopressin | Dp[Tyr(methyl)2,Arg8]-Vasopressin | Nelivaptan | Argipressin | Fedovapagon
相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Target-Focused Phenotypic Screening Library
Bioactivity
英文名: Mozavaptan
描述: Mozavaptan (OPC-31260) 是 benzazepine 衍生物，是一种竞争性加压素受体拮抗剂，作用于 V1 和 V2 受体，IC50 分别为 1.2 μM 和 14 nM。它可在体内拮抗精氨酸加压素的抗利尿作用，可用于低钠血症、抗利尿激素不适当综合征和充血性心力衰竭的研究。
激酶实验: 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].
体外活性: Mozavaptan (OPC-31260) 是一种非肽类、口服有效的竞争性抗利尿激素(AVP)抑制剂，具有25:1的V2至V1受体选择性比率，表明其相对于V2受体的选择性。[1] Mozavaptan (OPC-31260) 竞争性抑制AVP与V1和V2受体的结合。[2]
体内活性: Mozavaptan (OPC-31260) 在水负荷、醉酒麻醉的大鼠中，以剂量依赖的方式抑制了外源性AVP的抗利尿作用。在常规清醒大鼠中，经口给予1至30 mg/kg剂量的OPC-31260，能剂量依赖性地增加尿流并降低尿渗透压。[2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 22.5 mg/mL (52.63 mM)
关键字: AVP | OPC31260 | diuretic | Mozavaptan | hyponatremia | Nonpeptide | SIADH | OPC 31260 | inhibit | benzazepine | Vasopressin Receptor | arginine | vasopressin-V2 | Inhibitor
相关产品: OPC-51803 | Conopressin S acetate(111317-90-9 free base) | RG7713 | Val9-Oxytocin | Atosiban | Desmopressin | Dp[Tyr(methyl)2,Arg8]-Vasopressin | Nelivaptan | Argipressin | Fedovapagon
相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Target-Focused Phenotypic Screening Library
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