| 产品描述: | AKP-11 is an agonist of sphingosine-1-phosphate receptor 1 (S1P1) with an EC50 value of 0.047 μM for [35S]GTPγS binding to CHO-K1 cell membranes expressing the human receptor.1 It decreases surface expression of S1P1 and increases phosphorylation of Akt and ERK in CHO cells expressing S1P1-HA when used at a concentration of 100 nM.2 AKP-11 (1.3 and 3 mg/kg) reduces protein levels of IFN-γ and IL-17 in spinal cord tissue and decreases disease severity in a rat model of experimental autoimmune encephalomyelitis (EAE). It decreases peripheral counts of total lymphocytes and total, CD4+, CD8+, and CD26L+ T cells in an EAE rat model, as well as in health control animals, when administered at a dose of 1.3 mg/kg. |
| 靶点: |
S1P1 |
| 体内研究: |
S1P1 Agonist 1 (1.3mg/kg) attenuates EAE disease. EAE is the animal model of multiple sclerosis which is extensively used for investigating clinical studies for multiple sclerosis drugs. S1P1 Agonist 1 treatment reduces peripheral total blood lymphocyte and T lymphocyte counts significantly. The reduction in total lymphocytes and T cells are 48% and 41% in AKP-11 treated animals, respectively. The reduction in the CD4+ and CD8+ T cell populations are 41% and 40% in S1P1 Agonist 1 treated animals, respectively. S1P1 Agonist 1 treatment reduces CNS infiltration of T cells and Cytokines and enhances neuroprotection. S1P1 Agonist 1 treatment has little effect on the heart rate of animals. The decrease in blood pressure is also smaller with S1P1 Agonist 1 treatment as compared animals treated with FTY720. |
| 参考文献: |
1. Samuvel, D.J., Saxena, N., Dhindsa, J.S., et al. AKP-11 - A novel S1P1 agonist with favorable safety profile attenuates experimental autoimmune encephalomyelitis in rat model of multiple sclerosis. PLoS One 10(10):e0141781, (2015). |
| 溶解性: |
soluble in DMSO、DMF |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.253 ml |
11.264 ml |
22.529 ml |
| 5 mM |
0.451 ml |
2.253 ml |
4.506 ml |
| 10 mM |
0.225 ml |
1.126 ml |
2.253 ml |
| 50 mM |
0.045 ml |
0.225 ml |
0.451 ml |
|
| 注意: |
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