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唑喹达三盐酸盐  ≥98%

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包装规格：5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO(1mg/ml超声）水(5mg/ml超声)
产品描述：基本信息 产品编号： Z10081  产品名称： Zosuquidar trihydrochloride CAS: 167465-36-3   储存条件   粉末 -20℃ 四年 4℃ 二年 分子式： C32H31F2N3O2.3HCl 分子量： 636.99 化学名：  (R)-4-((1aR,6R,10bS)-1,2-Difluoro-1,1a,6,10b-tetrahydrodibenzo(a,e)cyclopropa(c)cycloheptan-6-yl)-alpha-((5-quinoloyloxy)methyl)-1-piperazineethanol,trihydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.5699mL 7.8494mL 15.6988mL 5mM 0.3140mL 1.5699mL 3.1398mL   生物活性 产品描述 P-糖蛋白(P-glycoprotein)抑制剂，Ki值为59nM。 靶点 Ki:59nM (P-glycoprotein).   体外研究 Zosuquidar completely or partially restores drug sensitivity in all P-gp-expressing leukemia cell lines and enhances the cytotoxicity of anthracyclines (daunorubicin,idarubicin,mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AmL blasts with active P-gp.In addition,P-gp inhibition by zosuquidar is found to be more potent than cyclosporine A in cells with highly active P-gp. 体内研究 Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain.An oral dose of 25mg/kg of zosuquidar trihydrochloride increases the brain concentrations by about 2.5-fold at 1h and 5-fold at 24h after paclitaxel administrationbarrier.Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner.Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6h after a 2mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20mg/kg zosuquidar.   推荐实验方法(仅供参考) 细胞实验:   Cells are cultured in 96-well plates. Each drug of interest is added at escalating concentrations in the presence or absence of either zosuquidar or CsA.After 48 hour incubation (except Mylotarg,4 days incubation),20μL of MTT is added to each well for a further 4 hour incubation.The purple precipitate is dissolved in 200μL DMSO,and the optic density (OD) is determined by the multi-well plate reader.   动物实验:   Rats:Female Sprague-Dawley rats are used in the study.Zosuquidar solutions are prepared in 5% mannitol and adjusted to pH 〜2.0 with concentrated HCl.Nelfinavir is infused (10mg/kg/h) for up to 10h with or without concurrent administration of an intravenous bolus dose of 2,6,or 20mg/kg zosuquidar given at 4h.Brain tissue and plasma are analyzed for both drug concentrations.             Mice:A stock solution of 5mg/mL of zosuquidar trihydrochloride is prepared in vehicle solution and diluted in sterile saline.The vehicle solution consisted of 20g/l mannitol and 1.5g/l of glycine in water for injection and adjusted to a pH of 2.7 with hydrochloric acid.P-gp knockout mice and wild type mice are used as a model for complete inhibition of P-gp.Zosuquidar trihydrochloride is administered orally at 25 and 80mg/kg 1h before i.v.paclitaxel and i.v.at 20mg/kg 10 min and 1h before paclitaxel.The concentrations of paclitaxel in plasma and tissues and of zosuquidar trihydrochloride in plasma are quantified by high-performance liquid chromatography.
保存条件：-20℃

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