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- 產(chǎn)品名稱(chēng)： Eliglustat hemitartrate 依利格魯司特酒石酸鹽
- 產(chǎn)品貨號(hào)： CST11176
- 貨期： 現(xiàn)貨
- 價(jià)格與訂購(gòu)： 1200
- 數(shù)量：
庫(kù)存： 5
- 規(guī)格： 100mg
- 產(chǎn)品信息
- 如何訂購(gòu)
產(chǎn)品描述
Eliglustat Hemitartrate, with an IC50 of 24 nM, is a specific, potent, oral active glucocerebral glycosidase inhibitor.
體外活性
Eliglustat tartrate shows good potency with an IC50 of 24 nM and specificity against the target enzyme.
體內(nèi)活性
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.
分子式
C27H42N2O10
分子量
554.63
別名
Genz-112638;依利格魯司特酒石酸鹽;Eliglustat tartrate
參考文獻(xiàn)
[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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儲(chǔ)存和溶解度
H2O:50 mg/mL (52.13 mM)
DMSO:50 mg/mL (52.13 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Note
For Research Use Only.
上一篇 EZM0414
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