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Celgosivir (MBI 3253) (Synonyms: MBI 3253; MDL 28574; MX3253)

Catalog No.GC32191

Celgosivir (MBI 3253) (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.

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Celgosivir (MBI 3253) Chemical Structure

Cas No.: 121104-96-9

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5mg
$153.00
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10mg
$248.00
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25mg
$522.00
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Sample solution is provided at 25 µL, 10mM.

Description of Celgosivir (MBI 3253)

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.

Protocol of Celgosivir (MBI 3253)

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.
[2]. Rathore AP, et al. Celgosivir treatment misfolds dengue virus NS1 protein, induces cellular pro-survival genes andprotects against lethal challenge mouse model. Antiviral Res. 2011 Dec;92(3):453-60.
[3]. Whitby K, et al. Action of celgosivir (6 O-butanoyl castanospermine) against the pestivirus BVDV: implications for the treatment of hepatitis C. Antivir Chem Chemother. 2004 May;15(3):141-51.
[4]. Watanabe S, et al. Dose- and schedule-dependent protective efficacy of celgosivir in a lethal mouse model for dengue virus infection informs dosing regimen for a proof of concept clinical trial. Antiviral Res. 2012 Oct;96(1):32-5.

Chemical Properties of Celgosivir (MBI 3253)

Cas No. 121104-96-9 SDF
Synonyms 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
Formula C12H21NO5 M.Wt 259.3
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Celgosivir (MBI 3253)

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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
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In vivo Formulation Calculator (Clear solution) of Celgosivir (MBI 3253)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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