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Celgosivir hydrochloride  ≥98%

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溶解性：溶于DMSO（100 mg/mL 超声)
产品描述：基本信息 产品编号：C10756 产品名称：Celgosivir hydrochloride CAS: 141117-12-6   储存条件 粉末 -20℃ 四年     分子式： C12H22ClNO5 溶于液体 -80℃ 六个月 分子量 295.76 -20℃ 一个月 化学名：  [(1S,6S,7S,8R,8aR)-1,7,8-trihydroxy-1,2,3,5,6,7,8,8a-octahydroindolizin-6-yl] butanoate;hydrochloride   Solubility (25°C)   体外 DMSO 100mg/mL (338.11mM; Need ultrasonic) Ethanol   Water ≥100mg/mL (338.11mM) 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 3.3811mL 16.9056mL 33.8112mL 5mM 0.6762mL 3.3811mL 6.7622mL 10mM 0.3381mL 1.6906mL 3.3811mL   生物活性 产品描述 α-葡萄糖苷酶 I抑制剂，在体外实验中的 IC50 值为 1.27μM。 靶点/IC50 α-glucosidase I IC50: 1.27μM   体外研究 Celgosivir is more effective (IC50=20μM) than the parent molecule (IC50=254μM) at causing the accumulation of glucosylated oligosaccharides in HIV-infected cells by inhibition of glycoprotein processing. Celgosivir exhibits potent antiviral activity against HIV-1 with an IC50 of 2.0±2.3μM. Bovine viral diarrhoea virus (BVDV) is a closely related virus of hepatitis C virus (HCV). Celgosivir inhibits BVDV with IC50 values of 16 and 47μM in plaque assay and cytopathic effect assay,respectively. Celgosivir inhibits DENV2 replication with an EC50 of 0.2μM. The EC50 values against DENV1, 3 and 4 are less than 0.7μM.   体内研究 Celgosivir fully protects AG129 mice from lethal infection with a mouse adapted dengue virus at a dose of 50 mg/kg twice daily (BID) for 5 days and is effective even after 48 h delayed treatment. The protection by celgosivir is dose- and scheduledependent and that a twice-a-day regimen of 50, 25 or 10mg/kg is more protective than a single daily dose of 100mg/kg.Pharmacokinetics studies of celgosivir in mice shows that it rapidly metabolizes to castanospermine. During primary infection with a mouse-adapted DENV strain S221, mice shows increased viremia on day 3, yet 80% survived day 10 with virus completely cleared by day 8.   推荐实验方法(仅供参考) 细胞实验:   Cell Assay The cytotoxicity of Celgosivir is measured by the Cell titer-Glo Luminescent cell viability assay. The luminescence signals for cells treated with the test compounds are compared to those for cells treated with the maximum tolerated DMSO to determine the 50% cytotoxic concentration.   动物实验:   Animal Administration Mice: To model ADE, mice are injected i.p. with 20μg /mouse of mouse monoclonal antibody against DENV E protein one day prior to infection. For treatment during infection, celgosivir (50mg/kg) is injected i.p. twice daily for 5 days, starting from day 0, 1 or 2. Blood is collected at days 1, 3 and 7 by submandibular bleeding. Survival of mice is followed until day 10 and survival curves are plotted.
保存条件：-20℃

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