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Eliglustat hemitartrate

Catalog No. T11176 CAS 928659-70-5

Synonyms: Genz-112638, Eliglustat tartrate

Eliglustat hemitartrate (Genz-112638) , with an IC50 of 24 nM, is a specific, potent, oral active glucocerebral glycosidase inhibitor.

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Eliglustat hemitartrate Chemical Structure

Eliglustat hemitartrate, CAS 928659-70-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 52.00
5 mg	In stock	$ 96.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 196.00
50 mg	In stock	$ 259.00
100 mg	In stock	$ 479.00
1 mL * 10 mM (in DMSO)	In stock	$ 136.00

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Purity: 99.1%

Biological Description

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Description	Eliglustat hemitartrate (Genz-112638) , with an IC50 of 24 nM, is a specific, potent, oral active glucocerebral glycosidase inhibitor.
Targets&IC50	Glucocerebroside synthase:24 nM
In vitro	Eliglustat tartrate shows good potency with an IC50 of 24 nM and specificity against the target enzyme.
In vivo	A novel inhibitor of glucosylceramide synthase (Genz-112638) and assessed its activity in a murine model of Gaucher disease (D409V/null).?Biochemical characterization of Genz-112638 showed good potency (IC(50) approximately 24nM) and specificity against the target enzyme.?Mice that received drug prior to significant accumulation of substrate (10 weeks of age) showed reduced levels of glucosylceramide and number of Gaucher cells in the spleen, lung and liver when compared to age-matched control animals.?Treatment of older mice that already displayed significant amounts of tissue glucosylceramide (7 months old) resulted in arrest of further accumulation of the substrate and appearance of additional Gaucher cells in affected organs.?These data indicate that substrate inhibition therapy with Genz-112638 represents a viable alternate approach to enzyme therapy to treat the visceral pathology in Gaucher disease.

Synonyms	Genz-112638, Eliglustat tartrate
Molecular Weight	959.17
Formula	C50H78N4O14
CAS No.	928659-70-5

Storage

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

Solubility Information

H2O: 50 mg/mL (52.13 mM)

DMSO: 50 mg/mL (52.13 mM)

References and Literature

1. McEachern KA, et al. A specific and potent inhibitor of glucosylceramide synthase for substrate inhibition therapy ofGaucher disease. Mol Genet Metab. 2007 Jul;91(3):259-67.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library FDA-Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Clinical Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Orally Active Compound Library

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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

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