Eliglustat (hemitartrate)
(Synonyms: 依利格鲁司特酒石酸盐,Genz-112638; Eliglustat tartrate) 目录号 : GC43595
A glucosylceramide synthase inhibitor
Cas No.:928659-70-5
Sample solution is provided at 25 µL, 10mM.
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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.
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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]. |
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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]. |
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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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| Cas No. | 928659-70-5 | SDF | |
| 别名 | 依利格鲁司特酒石酸盐,Genz-112638; Eliglustat tartrate | ||
| 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 | ||
| 分子式 | C23H36N2O4•1/2C4H6O6 | 分子量 | 479.6 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2) (1:30): 0.03 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet