Celgosivir (MBI 3253)
(Synonyms: MBI 3253; MDL 28574; MX3253) 目录号 : GC32191Celgosivir (MBI 3253) (MBI 3253; MDL 28574; MX3253) 是一种 α-葡萄糖苷酶 I 抑制剂;体外试验中抑制牛病毒性腹泻病毒 (BVDV),IC50 为 1.27 μM。
Cas No.:121104-96-9
Sample solution is provided at 25 µL, 10mM.
Celgosivir (MBI 3253; MDL 28574; MX3253) is a novel α-glucosidase I inhibitor, an enzyme that plays a critical role in viral maturation by initiating the processing of the N-linked oligosaccharides of viral envelope glycoproteins.[1]
The quantity of THP-1 cells is 1 × 105 , cells were washed once with media and replaced with 500 μl with a serial 4-fold dilution starting from 200 μM or 50 μM.[3]
Celgosivir, stored at 100 mg/ml in PBS at 30 °C, were diluted with PBS before each dosing to obtain 1 mg/200 μl (50 mg/kg) or 0.2 mg/200 μl (10 mg/kg). [3]
[1]. Durantel D. Celgosivir, an alpha-glucosidase I inhibitor for the potential treatment of HCV infection. Curr Opin Investig Drugs. 2009 Aug, 10(8):860-70. [2]. Whitby K et al. Action of celgosivir (6 O-butanoyl castanospermine) against the pestivirus BVDV: implications for thetreatment of hepatitis C. Antivir Chem Chemother, 2004 May, 15(3):141-51. [3]. Satoru Watanabe,Kitti Wing-Ki Chan et al. Optimizing celgosivir therapy in mouse models of dengue virus infection of serotypes 1 and 2: The search for a window for potential therapeutic efficacy. Antiviral Research, March 2016, Pages 10-19.
Cell experiment: | 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[3]. |
Animal experiment: | Mice: To model ADE, mice are injected i.p. with 20 μg /mouse of mouse monoclonal antibody against DENV E protein one day prior to infection. For treatment during infection, celgosivir (50 mg/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[3]. |
References: [1]. Taylor DL, et al. Inhibition of alpha-glucosidase I of the glycoprotein-processing enzymes by 6-O-butanoylcastanospermine (MDL 28,574) and its consequences in human immunodeficiency virus-infected T cells. Antimicrob Agents Chemother. 1994 Aug;38(8):1780-7. |
Cas No. | 121104-96-9 | SDF | |
别名 | MBI 3253; MDL 28574; MX3253 | ||
Canonical SMILES | O[C@@H]1[C@]2([H])[C@@H](O)[C@H](O)[C@@H](OC(CCC)=O)CN2CC1 | ||
分子式 | C12H21NO5 | 分子量 | 259.3 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.8565 mL | 19.2827 mL | 38.5654 mL |
5 mM | 0.7713 mL | 3.8565 mL | 7.7131 mL |
10 mM | 0.3857 mL | 1.9283 mL | 3.8565 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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