Mozavaptan-OPC-31260-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMozavaptanCat. No.: HY-18346CAS No.: 137975-06-5Synonyms: OPC-31260; OPC31260l分式: CHNO分量: 427.54作靶点: Vasopressin Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 6

2、.2 mg/mL (14.50 mM; Need warming)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3390 mL 11.6948 mL 23.3896 mL5 mM 0.4678 mL 2.3390 mL 4.6779 mL10 mM 0.2339 mL 1.1695 mL 2.3390 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Mozavaptan (OPC31260)有

3、服活性的肽阴道加压素(vasopressin)V2受体拮抗剂，其IC50值为14nM。IC50 & Target IC50: 14 nM (vasopressin receptor) 1体外研究Mozavaptan causes a competitive displacement of 3H-arginine vasopressin (AVP) binding to both V1 and1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEV2 receptors with IC50 values of 1.2 M and 14 nM, resp

4、ectively. The Kd of 3H-AVP is reduced significantlyin both rat liver and kidney in the presence of mozavaptan (Kd=1.1 nM in liver, Kd=1.38 nM in kidney) 1.体内研究 Mozavaptan at doses of 10 to 100 g/kg, i.v., inhibits the antidiuretic action of exogenously administeredarginine vasopressin in water-loade

5、d, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptandoes 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 30mg/kg in n

6、ormal conscious rats 1.PROTOCOLKinase Assay 1 To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasingconcentrations of 3H-AVP with or without excess (1 M) unlabelled AVP to obtain a saturation curve. Toinvestigate whether mozavaptan interacts competitiv

7、ely or noncompetitively, the saturation binding of 3H-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 M and 1 M in livermembranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted accordingto the method of Scatchard and fitted by a r

8、egression analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Mozavaptan is dissolved in DMSO at a concentration of 10 mM and diluted with assay buffer. FemaleAdministration 1 Brattleboro rats homozygous for hypothalamic diabetes ins

9、ipidus and weighing between 180 and 280g areused. Mozavaptan (30 mg/kg) and vehicle (5% gum arabic) are administered orally in a volume of 2 mL/kgand d(CH2)5Tyr(Et)VAVP (10pgkg-1) is administered in a volume of 1 mL/kg. Spontaneously voided urine iscollected for 6h with metabolic cages. Both before

10、and during the study, the rats received water and food adlibitum 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptorantagonist. Br J Pharmacol. 1992 Apr;105(4):787-91.McePdfHeightCaution: Product has not been fully v