Celgosivir hydrochloride|141117-12-6|(MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride)-陌孚医药/Medlife

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

目录号: PL04590 纯度: ≥98%

CAS No. :141117-12-6

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中文名称	Celgosivir hydrochloride
英文名称	Celgosivir hydrochloride
英文别名	Butanoic acid,(1S,6S,7S,8R,8aR)-octahydro-1,7,8-trihydroxy-6-indolizinyl ester, hydrochloride(1:1);[(1S,6S,7S,8R,8aR)-1,7,8-trihydroxy-1,2,3,5,6,7,8,8a-octahydroindolizin-6-yl] butanoate,hydrochloride;(1S,6S,7S,8R,8aR)-1,7,8-Trihydroxyoctahydro-6-indolizinyl Butyrate Hydrochloride;Butanoic acid, (1S,6S,7S,8R,8aR)-octahydro-1,7,8-trihydroxy-6-indolizinyl ester, hydrochloride;Castanospermine 6-O-Butyrate Hydrochloride;Celgosivir hydrochloride;MDL 28574A;MDL-28574A;Celgosivir (hydrochloride);Celgosivir HCl;MDL 28,574A;70U2NQU0FP;Celgosivir hydrochloride [USAN];[(1S,6S,7S,8R,8aR)-1,7,8-trihydroxy-1,2,3,5,6,7,8,8a-octahydroindolizin-6-yl] butanoate;hydrochloride;[(1S,6S,7S,8R,8aR)-1,7,8-trihydroxy-2,3,4,5,6,7,8,8a-octahydro-1H-indolizin-4-ium-6-yl] butanoate;chloride;Celgosivir hydrochloride (USAN);MX3253 hydrochloride;Castanospermine, 6-O-butyrate hydrochloride;MBI 3253 hydrochloride;MDL 28574
Cas No.	141117-12-6
分子式	C₁₂H₂₂ClNO₅
分子量	295.76
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC 50 of 1.27 μM in in vitro assay.

性状

Solid

IC50 & Target[1][2]

IC50: 1.27 μM (α-glucosidase I)

体外研究(In Vitro)

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 with an IC50 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 IC50 values of 16 and 47 μM in plaque assay and cytopathic effect assay, respectively. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Taylor DL, et al. Inhibition of alpha-glucosidase I of the glycoprotein-processing enzymes by 6-O-butanoylcastanospermine (MDL 28,574) and its consequences in human immunodeficiency virus-infected T cells. Antimicrob Agents Chemother. 1994 Aug;38(8):1780-
[2]. Whitby K, et al. Action of celgosivir (6 O-butanoyl castanospermine) against the pestivirus BVDV: implications for the treatment of hepatitis C. Antivir Chem Chemother. 2004 May;15(3):141-51.

溶解度数据	In Vitro: H₂O : ≥ 100 mg/mL (338.11 mM)DMSO : 100 mg/mL (338.11 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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