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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Eliglustat tartrate (GENZ-112638; Genz-99067; Cerdelga), the tartrate salt of eliglustat, is a specific and orally bioactive glucocerebroside synthase inhibitor (IC50 = 24 nM) that has been approved by the FDA in August 2014 for the treatment for Gaucher's disease type 1 (GD1). It is commonly used as the tartrate salt, the compound is believed to work by inhibition of glucosylceramide synthase. According to an article in Journal of the American Medical Association the oral substrate reduction therapy resulted in 'significant improvements in spleen volume, hemoglobin level, liver volume, and platelet count' in untreated adults with Gaucher disease Type 1.
| ln Vitro |
Eliglustat tartrate is selective for the target enzyme and has good efficacy, with an IC50 of 24 nM [1]. Dose-dependent results were obtained by incubating K562 or B16/F10 cells with escalating concentrations of Genz-112638 (0.6-1000 nM) for 72 hours. GM1 and GM3 levels on the cell surface decreased. In K562 cells, the average IC50 value for GM1 cell surface presentation inhibition was 24 nM (range 14-34 nM), while in B16/F10 cells, the average IC50 value for GM3 inhibition was 29 nM (range 12-48 nM) [1].
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| ln Vivo |
In comparison to age-matched control animals, mice administered the medication prior to considerable substrate accumulation (10 weeks of age) displayed lower levels of glucosylceramide and fewer Gaucher cells in the liver, lungs, and spleen [1].
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| 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
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| Molecular Formula |
2[C23H36N2O4].C4H6O6
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|---|---|
| Molecular Weight |
959.173
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| CAS # |
928659-70-5
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| Related CAS # |
Eliglustat;491833-29-5;Eliglustat-d15 tartrate;1884556-84-6
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| SMILES |
CCCCCCCC(N[C@H](CN1CCCC1)[C@@H](C2=CC=C(OCCO3)C3=C2)O)=O.CCCCCCCC(N[C@H](CN4CCCC4)[C@@H](C5=CC=C(OCCO6)C6=C5)O)=O.O=C(O)[C@H](O)[C@@H](O)C(O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~104.26 mM)
H2O : ≥ 50 mg/mL (~52.13 mM) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0426 mL | 5.2128 mL | 10.4257 mL | |
| 5 mM | 0.2085 mL | 1.0426 mL | 2.0851 mL | |
| 10 mM | 0.1043 mL | 0.5213 mL | 1.0426 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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