| Description | Celgosivir hydrochloride (MBI 3253 hydrochloride) is an α-glucosidase I inhibitor and inhibits bovine viral diarrhoea virus (BVDV) (IC50: 1.27 μM). |
| In vitro | Celgosivir is more effective (IC50: 20 μM) than the parent molecule (IC50: 254 μM) at causing the accumulation of glucosylated oligosaccharides in HIV-infected cells by inhibition of glycoprotein processing. Celgosivir exhibits potent antiviral activity against HIV-1 (IC50: 2.0 μM) [1]. BVDV is a closely related virus of hepatitis C virus (HCV). Celgosivir inhibits BVDV with IC50 values of 16 and 47 μM in plaque assay and cytopathic effect assay, respectively [2]. Celgosivir inhibits DENV2 replication with an EC50 of 0.2 μM. The EC50 values against DENV1, 3, and 4 are less than 0.7 μM [3]. |
| In vivo | During primary infection with a mouse-adapted DENV strain S221, mice show increased viremia on day 3, yet 80% survived day 10 with a virus completely cleared by day 8 [3]. Celgosivir (50 mg/kg, BID for 5 days) fully protects AG129 mice from lethal infection with a mouse-adapted dengue virus and is effective even after 48 h delayed treatment. The protection by celgosivir is dose- and schedule-dependent and that a twice-a-day regimen of 50, 25, or 10 mg/kg is more protective than a single daily dose of 100 mg/kg. Pharmacokinetics studies of celgosivir in mice show that it rapidly metabolizes to castanospermine [4]. |
| Target activity | α-glucosidase I:1.27 μM |
| Synonyms | MX3253 hydrochloride, MBI 3253 hydrochloride, MDL 28574 hydrochloride |
| molecular weight | 295.76 |
| Molecular formula | C12H22ClNO5 |
| CAS | 141117-12-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: 100 mg/mL (338.11 mM) DMSO: 100 mg/mL (338.11 mM), Sonication is recommended. |
| 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. |