| 产品描述： | Amiselimod hydrochloride is a sphingosine 1-phosphate receptor-1 (S1P1) modulator |
| 靶点： |
S1P Receptor;LPL Receptor;S1PReceptor; LPLReceptor |
| 体内研究： |
After oral administration of amiselimod or fingolimod at 1 mg/kg, the concentration of amiselimod-P in rat heart tissue was relatively lower than that of fingolimod-P, potentially contributing to the minimal cardiac effects of amiselimod. Amiselimod-P showed potent selectivity for S1P1, high selectivity for S1P5, minimal agonist activity for S1P4, no distinct agonist activity for S1P2 or S1P3, and approximately 5-fold weaker GIRK activation than fingolimod-P. Amiselimod 0·2 mg and 0·4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions |
| 参考文献： |
1. Sugahara K et al. Amiselimod, a novel sphingosine 1-phosphate receptor-1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk. Br J Pharmacol. 2016 Oct 7. 2. Kappos L et al. Safety and efficacy of amiselimod in relapsing multiple sclerosis (MOMENTUM): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet Neurol. 2016 Oct;15(11):1148-59. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.416 ml |
12.08 ml |
24.16 ml |
| 5 mM |
0.483 ml |
2.416 ml |
4.832 ml |
| 10 mM |
0.242 ml |
1.208 ml |
2.416 ml |
| 50 mM |
0.048 ml |
0.242 ml |
0.483 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京