Celgosivir 是 α-葡萄糖苷酶 I (α-Glucosidase I) 抑制剂，在体外实验中的 IC50 值为 1.27 μM。

Celgosivir is an inhibitor of α-glucosidase I. In vitro assay, it inhibits bovine viral diarrhoea virus (BVDV) ( IC50: 1.27 μM ).

Celgosivir exhibits potent antiviral activity against HIV-1 (IC50: 2.0±2.3 μM) [1]. Celgosivir inhibits DENV2 replication (EC50: 0.2 μM). The EC50 values against DENV1, 3 and 4 are less than 0.7 μM[3]. 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. Bovine viral diarrhoea virus (BVDV) is a closely related virus of hepatitis C virus (HCV). In plaque assay and cytopathic effect assay, Celgosivir inhibits BVDV, with IC50 values of 16 and 47 μM , respectively[2].

Celgosivir fully protects AG129 mice from lethal infection with a mouse adapted dengue virus at a dose of 50 mg/kg twice daily (BID) for 5 days. Which 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. During primary infection with a mouse-adapted DENV strain S221. The mice shows increased viremia on day 3, yet 80% survived day 10 with virus completely cleared by day 8[3].

121104-96-9

C12H21NO5

259.3

MX3253;MBI 3253;MDL 28574;6 O-butanoyl castanospermine;Celgosivir

H2O:1.8mg/mL (6.9mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years