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Celgosivir

CAS No. : 121104-96-9

MCE 国际站：Celgosivir

产品活性：Celgosivir (MBI 3253; MDL 28574; MX3253) 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。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Glucosidase  |  HCV  |  HIV

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 with an IC₅₀ of 2.0±2.3 μM. Bovine viral diarrhoea virus (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. 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.

In Vivo: 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 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 shows that it rapidly metabolizes to castanospermine. During primary infection with a mouse-adapted DENV strain S221, mice shows increased viremia on day 3, yet 80% survived day 10 with virus completely cleared by day 8.

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货号: HY-16134

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