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5mg |
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25mg |
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50mg |
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100mg |
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Purity: ≥98%
Eliglustat (GENZ-112638, Genz-99067, GENZ112638, Genz99067, Cerdelga) is a novel, potent, specific and orally bioactive glucocerebroside synthase inhibitor (IC50 = 24 nM) approved by FDA in 2014 for the treatment for Gaucher's disease.
ln Vitro |
Eliglustat tartrate has the ability to inhibit target enzymes and has good potency, with an IC50 of 24 nM [1]. The addition of Genz-112638 (0.6-1000 nM) to K562 or B16/F10 cells over a period of 72 hours led in a delayed suppression of GM1 and GM3 cell surfaces, with an average IC50 of 24 nM (range 14-1000 nM) in K562 cells. 34 nM), with an average IC50 value for GM3 inhibition in B16/F10 cells of 29 nM (range 12-34 nM). 48 nanometers)[1].
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ln Vivo |
In comparison to age-matched control animals, mice with a significant accumulation of substrate prior to therapy had lower levels of step ceramide and fewer Gaucher cells in their spleen, lung, and heart [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):259-68
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Molecular Formula |
C23H36N2O4
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Molecular Weight |
404.551
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Exact Mass |
404.2675
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CAS # |
491833-29-5
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Related CAS # |
Eliglustat hemitartrate;928659-70-5;Eliglustat-d15 tartrate;1884556-84-6;Eliglustat-d4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
InChI=1S/C23H36N2O4/c1-2-3-4-5-6-9-22(26)24-19(17-25-12-7-8-13-25)23(27)18-10-11-20-21(16-18)29-15-14-28-20/h10-11,16,19,23,27H,2-9,12-15,17H2,1H3,(H,24,26)/t19-,23-/m1/s1
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InChi Key |
N-((1R,2R)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)octanamide
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InChi Code |
FJZZPCZKBUKGGU-AUSIDOKSSA-N
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Chemical Name |
Genz-99067 GENZ-112638Cerdelga Genz99067 UNIIN0493335P3GENZ 112638Genz 99067 GENZ112638 Eliglustat tartrate eliglustat hemitartrate Eliglustat trade name Cerdelga.
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HS Tariff Code |
2934.99.9001
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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 (~247.19 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4719 mL | 12.3594 mL | 24.7188 mL | |
5 mM | 0.4944 mL | 2.4719 mL | 4.9438 mL | |
10 mM | 0.2472 mL | 1.2359 mL | 2.4719 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.