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141117-12-6

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141117-12-6

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CAS No. 141117-12-6

分子式 C12H22ClNO5

分子量 295.76

英文名称 Celgosivir (hydrochloride)

中文同义词化合物 T10755

基本信息

产品名称

141117-12-6

中文同义词

化合物 T10755

英文名称

Celgosivir (hydrochloride)

英文同义词

Celgosivir (hydrochloride);MBI 3253 hydrochloride;MDL 28574 hydrochloride;MX3253 hydrochloride

CAS No.

141117-12-6

分子式

C12H22ClNO5

分子量

295.76

EINECS号

MDL NO.

MFCD30738181

MOL

141117-12-6.mol

性质

形态

固体

颜色

白色至灰色

储存条件

Store at -20°C

水溶解性

Water : ≥ 200 mg/mL (676.22 mM)

用途

靶点

IC50: 1.27 μM (α-glucosidase I)

体内研究

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.

体外研究

Celgosivir is more effective (IC 50 =20 μM) than the parent molecule (IC 50 =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 IC 50 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 IC 50 values of 16 and 47 μM in plaque assay and cytopathic effect assay, respectively. Celgosivir inhibits DENV2 replication with an EC 50 of 0.2 μM. The EC 50 values against DENV1, 3 and 4 are less than 0.7 μM.

生物活性

Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) 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。

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