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141117-12-6

中文名稱 141117-12-6
英文名稱 Celgosivir (hydrochloride)
CAS 141117-12-6
分子式 C12H22ClNO5
分子量 295.76
MOL 文件 141117-12-6.mol
更新日期 2024/12/03 15:40:33
141117-12-6 結(jié)構(gòu)式 141117-12-6 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10755
英文別名
MX3253 hydrochloride
MBI 3253 hydrochloride
MDL 28574 hydrochloride
Celgosivir (hydrochloride)

物理化學性質(zhì)

儲存條件-20°C儲存
形態(tài)Solid
顏色White to gray
水溶解性Water : ≥ 200 mg/mL (676.22 mM)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
141117-12-6價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-16134A141117-12-6
Celgosivir hydrochloride
141117-12-61mg1500元
2024/11/08HY-16134A141117-12-6
Celgosivir hydrochloride
141117-12-65mg3500元
2024/11/08HY-16134A141117-12-6
Celgosivir hydrochloride
141117-12-610mM * 1mLin DMSO4880元

常見問題列表

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) 抑制劑,在體外實驗中的 IC50 值為 1.27 μM。
靶點

IC50: 1.27 μM (α-glucosidase I)

體外研究

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.

體內(nèi)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.

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