| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Celgosivir hydrochloride targets alpha-glucosidase I, an enzyme involved in the processing of N-linked glycoproteins. alpha-Glucosidase I catalyzes the removal of the terminal glucose residue from the lipid-linked oligosaccharide precursor during glycoprotein biosynthesis. By inhibiting alpha-glucosidase I, celgosivir disrupts the proper folding and processing of viral glycoproteins, leading to the accumulation of glucosylated oligosaccharides. This inhibition prevents the production of infectious viral particles and reduces viral replication. The compound's mechanism of action involves inhibition of glycoprotein processing in virus-infected cells.
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| 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].
Celgosivir hydrochloride demonstrates potent in vitro antiviral activity against multiple viruses. The compound inhibits BVDV with an IC50 of 1.27 microM in in vitro assays. Celgosivir is more effective (IC50=20 microM) than the parent molecule (IC50=254 microM) 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+/-2.3 microM. Celgosivir inhibits BVDV with IC50 values of 16 and 47 microM in plaque assay and cytopathic effect assay, respectively. Celgosivir inhibits DENV2 replication with an EC50 of 0.2 microM, and EC50 values against DENV1, 3 and 4 are less than 0.7 microM. |
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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].
In vivo, Celgosivir hydrochloride has demonstrated significant antiviral efficacy. Celgosivir fully protects AG129 mice from lethal infection with a mouse adapted dengue virus at a dose of 50 mg/kg and is effective even after 48 h delayed treatment. Pharmacokinetics studies of celgosivir in mice show that it rapidly metabolizes to castanospermine. During primary infection with a mouse-adapted DENV strain S221, mice show increased viremia on day 3, yet 80% survive day 10 with virus completely cleared by day 8. The compound's ability to protect against lethal dengue virus infection in animal models supports its potential for antiviral research. |
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| Cell Assay |
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| Animal Protocol |
In vivo animal studies for Celgosivir hydrochloride are conducted using mouse models of dengue virus infection. AG129 mice (interferon alpha/beta and gamma receptor-deficient) are infected with a mouse-adapted dengue virus strain. Celgosivir is administered via intraperitoneal injection or oral gavage at various doses (e.g., 50 mg/kg) and schedules. Survival is monitored, and viral loads in serum and tissues are measured by plaque assay or qRT-PCR. Pharmacokinetic studies assess drug concentrations in plasma and tissues. To mimic antibody-dependent enhancement (ADE), mice may be injected with monoclonal antibody against the DENV E protein one day before infection. Efficacy is expressed as survival rate and reduction in viral load compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Celgosivir hydrochloride have been characterized in preclinical studies. The compound has a molecular formula of C12H22ClNO5 and a molecular weight of 295.76 g/mol. Celgosivir rapidly metabolizes to castanospermine in mice. The compound is highly soluble in water (≥200 mg/mL) and is soluble in DMSO. Celgosivir hydrochloride has good oral bioavailability. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's solubility and oral bioavailability support its use in preclinical studies of antiviral efficacy. Storage should be in a cool and dry place.
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| Toxicity/Toxicokinetics |
Celgosivir hydrochloride is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As an alpha-glucosidase inhibitor, the compound would be expected to have effects on glycoprotein processing in host cells. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound has shown promise in the treatment of flavivirus infections. Celgosivir hydrochloride is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
Celgosivir hydrochloride (MBI 3253 hydrochloride, MDL 28574A) is an alpha-glucosidase I inhibitor with significant antiviral activity. It inhibits BVDV with an IC50 of 1.27 microM. The compound has a molecular formula of C12H22ClNO5 and a molecular weight of 295.76 g/mol. Celgosivir hydrochloride has shown promise in the treatment of flavivirus infections, including dengue and hepatitis C virus (HCV), by inhibiting viral replication. Celgosivir fully protects AG129 mice from lethal dengue virus infection at a dose of 50 mg/kg. The compound has not entered clinical trials for all indications and is available from research chemical suppliers for non-clinical research purposes only.
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| Molecular Formula |
C12H22CLNO5
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| Molecular Weight |
295.7598
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| Exact Mass |
295.119
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| CAS # |
141117-12-6
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| Related CAS # |
Celgosivir;121104-96-9
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| PubChem CID |
3033824
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| Appearance |
White to gray solid powder
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| Boiling Point |
422.9ºC at 760 mmHg
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| Flash Point |
209.6ºC
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| Vapour Pressure |
6.34E-09mmHg at 25°C
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
311
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CCCC(=O)O[C@H]1CN2CC[C@@H]([C@@H]2[C@H]([C@@H]1O)O)O.Cl
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| InChi Key |
KXNZMBFOWDNCRU-QVMZSJACSA-N
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| InChi Code |
InChI=1S/C12H21NO5.ClH/c1-2-3-9(15)18-8-6-13-5-4-7(14)10(13)12(17)11(8)16;/h7-8,10-12,14,16-17H,2-6H2,1H3;1H/t7-,8-,10+,11+,12+;/m0./s1
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| Chemical Name |
[(1S,6S,7S,8R,8aR)-1,7,8-trihydroxy-1,2,3,5,6,7,8,8a-octahydroindolizin-6-yl] butanoate;hydrochloride
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| HS Tariff Code |
2934.99.9001
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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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