Celgosivir hydrochloride, Inhibitor

Celgosivir hydrochloride

Cat. Num. AAA5752899

• Purity: 98.00%
• Synonyms: Celgosivir hydrochloride; MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: H2O: 100mg/mL (338.11mM); DMSO: 100mg/mL (338.11mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C12H22ClNO5
• SMILES: O[C@@H]1[C@]2([H])[C@@H](O)[C@H](O)[C@@H](OC(CCC)=O)CN2CC1.Cl[H]
• CAS Number: 141117-12-6
• Target & IC50: alpha-glucosidase I: ic50 1.27uM
• In Vitro: 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 (50mg/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 10mg/kg is more protective than a single daily dose of 100mg/kg. Pharmacokinetics studies of celgosivir in mice show that it rapidly metabolizes to castanospermine [4].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Celgosivir hydrochloride, inhibitor

Celgosivir hydrochloride (MBI 3253 hydrochloride) is an alpha-glucosidase I inhibitor and inhibits bovine viral diarrhoea virus (BVDV) (IC50: 1.27 uM).

References

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.
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.
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.
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.
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.
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.
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.
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.