CELGOSIVIR
|
|
|
- CAS號:
- 121104-96-9
- 英文名:
- celgosivir
- 英文別名:
- BuCast;MX3253;MBI 3253;MDL 28574;celgosivir;Celgosivir (free base);6-O-butyl castanospermine;6-Butyryl castanospermine;Castanospermine 6-butyrate;MDL28574;MDL-28574;MDL 28574
- 中文名:
- CELGOSIVIR
- 中文別名:
- 西戈斯韋;化合物 T10755L;CELGOSIVIR, Α-葡萄糖苷酶抑制劑
- CBNumber:
- CB51074377
- 分子式:
- C12H21NO5
- 分子量:
- 259.3
- MOL File:
- 121104-96-9.mol
|
|
|
CELGOSIVIR化學性質
-
熔點:
-
114-115 °C
-
|
-
沸點:
-
422.9±45.0 °C(Predicted)
-
|
-
密度:
-
1.33±0.1 g/cm3(Predicted)
-
|
-
儲存條件:
-
Hygroscopic, -20°C Freezer, Under inert atmosphere
-
|
-
溶解度:
-
Chloroform (Slightly), DMSO (Slightly)
-
|
-
形態(tài):
-
Solid
-
|
-
酸度系數(pKa):
-
13.14±0.70(Predicted)
-
|
-
顏色:
-
White to Pale Beige
-
|
-
穩(wěn)定性:
-
Hygroscopic
-
|
CELGOSIVIR性質、用途與生產工藝
Celgosivir (MBI 3253; MDL 28574; MX3253) 是 α-葡萄糖苷酶 I (α-glucosidase I) 抑制劑，在體外實驗中的 IC50 值為 1.27 μM。
IC50: 1.27 μM (α-glucosidase I)
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.
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.
CELGOSIVIR
上下游產品信息
上游原料
下游產品
121104-96-9, CELGOSIVIR 相關搜索:
- 抑制劑
- 標準品 -中藥標準品
- 植物提取物
- CELGOSIVIR, Α-葡萄糖苷酶抑制劑
- 西戈斯韋
- 化合物 T10755L
- 121104-96-9
- Celgosivir (free base)
- 6-O-butyl castanospermine
- Butanoic acid, (1S,6S,7S,8R,8aR)-octahydro-1,7,8-trihydroxy-6-indolizinyl ester
- MX3253
- MBI 3253
- MDL28574;MDL-28574;MDL 28574
- BuCast
- Castanospermine 6-butyrate
- 6-Butyryl castanospermine
- (1S)-1,2,3,5,6,7,8,8aα-Octahydro-6α-butyryloxyindolizine-1β,7β,8α-triol
- MDL 28574
- celgosivir