化合物 T10755 T10755

Product Introduction
Bioactivity


英文名: Celgosivir hydrochloride

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

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 100 mg/mL (338.11 mM)
DMSO : 100 mg/mL (338.11 mM)


关键字: Celgosivir hydrochloride | MBI-3253 Hydrochloride | MX-3253 Hydrochloride | MX3253 Hydrochloride | MDL 28574 Hydrochloride | MDL-28574 Hydrochloride | MX 3253 Hydrochloride | MBI 3253 Hydrochloride | Celgosivir Hydrochloride | MBI3253 Hydrochloride | MDL28574 Hydrochloride

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途