| 產品描述： | Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM |
| 靶點： |
IC50: 24 nM (glucocerebroside synthase);Transferase |
| 體外研究： |
Eliglustat tartrate shows good potency with an IC50 of 24 nM and specificity against the target enzyme.Incubating K562 or B16/F10 cells for 72 h with increasing amounts of Genz-112638 (0.6-1000 nM) results in a dose-dependent reduction of cell surface levels of both GM1 and GM3. The mean IC50 value for inhibiting the cell surface presentation of GM1 in K562 cells was 24 nM (range 14-34 nM) and that for GM3 in B16/F10 cells was 29 nM (range 12-48 nM) |
| 體內研究： |
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 |
| 參考文獻： |
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. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-80℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.472 ml |
12.36 ml |
24.719 ml |
| 5 mM |
0.494 ml |
2.472 ml |
4.944 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.472 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.494 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京