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Mozavaptan Sale

(Synonyms: 莫扎伐普坦,OPC-31260) 目录号 : GC14880

Mozavaptan (OPC-31260) 是一种苯并氮杂类衍生物,是一种有效的、选择性的、竞争性的、具有口服活性的加压素 V2 受体拮抗剂,IC50 为 14 nM。

Mozavaptan Chemical Structure

Cas No.:137975-06-5

规格 价格 库存 购买数量
10mg
¥305.00
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100mg
¥2,340.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

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].

Animal experiment:

Rats: Mozavaptan is dissolved in DMSO at a concentration of 10 mM and diluted with assay buffer. Female Brattleboro rats homozygous for hypothalamic diabetes insipidus and weighing between 180 and 280g are used. Mozavaptan (30 mg/kg) and vehicle (5% gum arabic) are administered orally in a volume of 2 mL/kg and d(CH2)5Tyr(Et)VAVP (10pgkg-1) is administered in a volume of 1 mL/kg. Spontaneously voided urine is collected for 6h with metabolic cages. Both before and during the study, the rats received water and food ad libitum[1].

References:

[1]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.

产品描述

Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM.

Mozavaptan causes a competitive displacement of [3H]-arginine vasopressin (AVP) binding to both V1 and V2 receptors with IC50 values of 1.2 μM and 14 nM, respectively. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of mozavaptan (Kd=1.1 nM in liver, Kd=1.38 nM in kidney)[1].

Mozavaptan at doses of 10 to 100 μg/kg, i.v., inhibits the antidiuretic action of exogenously administered arginine vasopressin in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptan does not exert an antidiuretic activity suggesting that it is not a partial V2 receptor agonist. Mozavaptan dose-dependently increases urine flow and decreases urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats[1].

References:
[1]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.

Chemical Properties

Cas No. 137975-06-5 SDF
别名 莫扎伐普坦,OPC-31260
化学名 N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
Canonical SMILES CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C
分子式 C27H29N3O2 分子量 427.54
溶解度 Limited solubility 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.339 mL 11.6948 mL 23.3896 mL
5 mM 0.4678 mL 2.339 mL 4.6779 mL
10 mM 0.2339 mL 1.1695 mL 2.339 mL
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