中文名 | Celgosivir |
英文名 | Celgosivir |
别名 | 化合物 T10755L |
英文别名 | MBI 3253 MDL28574 MDL-28574 MDL 28574 celgosivir Celgosivir (1S)-1,2,3,5,6,7,8,8aα-Octahydro-6α-butyryloxyindolizine-1β,7β,8α-triol |
CAS | 121104-96-9 |
化学式 | C12H21NO5 |
分子量 | 259.3 |
密度 | 1.33±0.1 g/cm3(Predicted) |
熔点 | 114-115 °C |
沸点 | 422.9±45.0 °C(Predicted) |
溶解度 | 氯仿 (微溶) 、DMSO (微溶) |
酸度系数 | 13.14±0.70(Predicted) |
存储条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Pale Beige |
MDL号 | MFCD00886617 |
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. |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.857 ml | 19.283 ml | 38.565 ml |
5 mM | 0.771 ml | 3.857 ml | 7.713 ml |
10 mM | 0.386 ml | 1.928 ml | 3.857 ml |
5 mM | 0.077 ml | 0.386 ml | 0.771 ml |
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