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Celgosivir  

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包装规格：5mg in glass bottle
溶解性：溶于水(2mg/mL)
产品描述：基本信息 产品编号： C11213 产品名称： Celgosivir CAS: 121104-96-9   储存条件 粉末 -20℃ 四年     分子式： C12H21NO5 溶于液体     分子量 259.30     化学名：  Butanoic acid [1S-(1α,6β,7α,8β,8aβ)]-octahydro-1,7,8-trihydroxy-6-indolizinyl ester 生物活性 产品描述 一种α-葡萄糖苷酶I(α-glucosidaseI)抑制剂。 靶点 IC50: 1.27μM (α-glucosidase I) 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 50mg/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) 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     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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