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Eliglustat (hemitartrate) (Synonyms: Genz-112638)

Catalog No.GC43595

L'éliglustat (hémitartrate) est un inhibiteur de la glucocérébroside synthase spécifique, puissant et actif par voie orale avec une IC50 de 24 nM.

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Eliglustat (hemitartrate) Chemical Structure

Cas No.: 928659-70-5

Taille Prix Stock Qté
1mg
21,00 $US
En stock
5mg
95,00 $US
En stock
10mg
140,00 $US
En stock
25mg
366,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

The inhibitory activity of Genz-112638 is determined indirectly by measuring its effect on the cell surface levels of the gangliosides GM1 and GM3 on either K562 or B16/F10 cells. GM1 levels on the K562 cells are determined by incubating the cells with increasing amounts of Genz-112638 (0.6-1000 nM) for 72 h after which the cells are harvested and stained using 10 μg of recombinant cholera toxin-FITC in 100 μL phosphate buffered saline (PBS) containing 0.5% bovine serum albumin (BSA) for 30 min on ice. Cells are ished, resuspended in PBS containing 0.5% BSA and the fluorescence quantitated[1].

Animal experiment:

Mice: Eliglustat hemitartrate is dissolved in water for injection and administered in a dose escalation from 75 mg/kg/day to 150 mg/kg/day over the course of nine days, with three days at each dose and increments of 25 mg/kg/day. Mice are weighed three times per week to monitor the potential impact of the drug on their overall health. Animals are killed by carbon dioxide inhalation[1].

References:

[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.

Background

Eliglustat is a potent and selective inhibitor of glucosylceramide synthase with an IC50 value of 40 nM for the reduction of glucosylceramide synthesis in K562 cells. Inhibition of glucosylceramide synthase, the rate-limiting enzyme in glycosphingolipid synthesis, also reduces production of cell surface gangliosides GM1 and GM3 on K562 and B16/F10 cells, with IC50 values of 24 and 29 nM, respectively. Eliglustat is specific to glucosylceramide synthase over similar enzymes, having minimal activity (IC50 = >10 μM) at α-glucosidase I and II, lysosomal glucocerebrosidase (GBA1), non-lysosomal glucosylceramidase (GBA2), sucrase, and maltase. In vivo, eliglustat induces a dose-dependent decrease in glucosylceramide accumulation in the liver and lungs of D409V/null mice, a model of Gaucher disease. It also prevents further glucosylceramide accumulation if administered after liver and lung deposits have been established.

Chemical Properties

Cas No. 928659-70-5 SDF
Synonymes Genz-112638
Canonical SMILES O[C@@H]([C@H](N([H])C(CCCCCCC)=O)CN1CCCC1)C2=CC=C(OCCO3)C3=C2.OC([C@H](O)[C@@H](O)C(O)=O)=O.O[C@@H]([C@H](N([H])C(CCCCCCC)=O)CN4CCCC4)C5=CC=C(OCCO6)C6=C5
Formula C23H36N2O4•1/2C4H6O6 M.Wt 479.6
Solubility DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2) (1:30): 0.03 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.0851 mL 10.4254 mL 20.8507 mL
5 mM 0.417 mL 2.0851 mL 4.1701 mL
10 mM 0.2085 mL 1.0425 mL 2.0851 mL
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Review for Eliglustat (hemitartrate)

Average Rating: 5 ★★★★★ (Based on Reviews and 35 reference(s) in Google Scholar.)

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