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Celgosivir hydrochloride

Catalog No. T10755 CAS 141117-12-6

Synonyms: MX3253 hydrochloride, MBI 3253 hydrochloride, MDL 28574 hydrochloride

Celgosivir hydrochloride (MBI 3253 hydrochloride) is an α-glucosidase I inhibitor and inhibits bovine viral diarrhoea virus (BVDV) (IC50: 1.27 μM).

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Celgosivir hydrochloride Chemical Structure

Celgosivir hydrochloride, CAS 141117-12-6

Pack Size	Availability	Price/USD
2 mg	5 days	$ 215.00
25 mg	8-10 weeks	$ 1,370.00
50 mg	8-10 weeks	$ 1,790.00
100 mg	8-10 weeks	$ 2,710.00
1 mL * 10 mM (in DMSO)	5 days	$ 485.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Celgosivir hydrochloride (MBI 3253 hydrochloride) is an α-glucosidase I inhibitor and inhibits bovine viral diarrhoea virus (BVDV) (IC50: 1.27 μM).
Targets&IC50	α-glucosidase I:1.27 μM
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 (IC50: 2.0 μM) [1]. 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 [2]. 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 [3].
In vivo	During primary infection with a mouse-adapted DENV strain S221, mice show increased viremia on day 3, yet 80% survived day 10 with a virus completely cleared by day 8 [3]. Celgosivir (50 mg/kg, BID for 5 days) fully protects AG129 mice from lethal infection with a mouse-adapted dengue virus 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 show that it rapidly metabolizes to castanospermine [4].

Synonyms	MX3253 hydrochloride, MBI 3253 hydrochloride, MDL 28574 hydrochloride
Molecular Weight	295.76
Formula	C12H22ClNO5
CAS No.	141117-12-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (338.11 mM)

DMSO: 100 mg/mL (338.11 mM), Sonification is recommended.

References and Literature

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):1780-7. 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. 3. Watanabe S, et al. Dose- and schedule-dependent protective efficacy of celgosivir in a lethal mouse model for dengue virus infection informs dosing regimen for a proof of concept clinical trial. Antiviral Res. 2012 Oct;96(1):32-5. 4. Rathore AP, et al. Celgosivir treatment misfolds dengue virus NS1 protein, induces cellular pro-survival genes andprotects against lethal challenge mouse model. Antiviral Res. 2011 Dec;92(3):453-60.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Celgosivir hydrochloride 141117-12-6 Others MX3253 hydrochloride MBI-3253 Hydrochloride MX-3253 Hydrochloride MX3253 Hydrochloride MDL 28574 Hydrochloride MDL-28574 Hydrochloride MX 3253 Hydrochloride MBI 3253 Hydrochloride MBI 3253 hydrochloride MDL 28574 hydrochloride Celgosivir Hydrochloride MBI3253 Hydrochloride MDL28574 Hydrochloride inhibitor inhibit

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