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Celgosivir hydrochloride (MDL-28574A) is a novel and potent α-glucosidase I inhibitor that inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
| ln Vitro |
By inhibiting glycoprotein processing, cegosivir is more effective (IC50=20 μM) than the parent molecule (IC50=254 μM) at causing the buildup of glucosylated oligosaccharides in HIV-infected cells. With an IC50 of 2.0±2.3 μM, celibosivir demonstrates strong antiviral activity against HIV-1[1]. The hepatitis C virus (HCV) and the bovine viral diarrhea virus (BVDV) are closely related viruses. With IC50 values of 16 and 47 μM in the plaque assay and cytopathic effect assay, respectively, celgosivir suppresses BVDV[2]. With an EC50 of 0.2 μM, celgosivir suppresses the replication of DENV2. Less than 0.7 μM is the EC50 value against DENV1, 3, and 4[3].
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| ln Vivo |
At a dose of 50 mg/kg twice daily (BID) for five days, cegosivir completely protects AG129 mice against a deadly infection with a mouse-adapted dengue virus. It remains efficacious even after a 48-hour treatment delay. Celgosivir's protective effects vary depending on the dose and schedule; a 50, 25 or 10 mg/kg twice-day regimen is more effective than a 100 mg/kg dose taken once daily. Celgosivir quickly metabolizes to castanospermine, according to pharmacokinetic tests conducted in mice[4]. When mice were first infected with the mouse-adapted DENV strain S221, their viremia increased on day 3, but by day 10, 80% of them had recovered, and by day 8, the virus had totally disappeared[3].
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| 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]. 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. [3]. 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. [4]. 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 |
| Molecular Formula |
C12H22CLNO5
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|---|---|
| Molecular Weight |
295.7598
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| CAS # |
141117-12-6
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| Related CAS # |
Celgosivir;121104-96-9
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| SMILES |
Cl[H].O([H])[C@@]1([H])[C@@]([H])([C@]([H])(C([H])([H])N2C([H])([H])C([H])([H])[C@@]([H])([C@@]21[H])O[H])OC(C([H])([H])C([H])([H])C([H])([H])[H])=O)O[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~338.11 mM)
DMSO : ~100 mg/mL (~338.11 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (338.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3811 mL | 16.9056 mL | 33.8112 mL | |
| 5 mM | 0.6762 mL | 3.3811 mL | 6.7622 mL | |
| 10 mM | 0.3381 mL | 1.6906 mL | 3.3811 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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