| Bioactivity | S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities. | ||||||||||||
| Target | S1P1 | ||||||||||||
| Invitro | S1P1 Agonist 1 binds to S1P1 is internalized and activates intracellular AKT and ERKs cellular signaling pathways. S1P1 Agonist 1 mediated S1P1 downregulation is independent of sphingosine kinase activity indicating it to be a direct agonist of S1P1. S1P1 Agonist 1 decreases cell surface expression of S1P1 in in vitro cell culture model[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> S1P1 agonist 1 相关抗体: | ||||||||||||
| In Vivo | 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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
| CAS | 1220973-37-4 | ||||||||||||
| Formula | C22H22ClN3O5 | ||||||||||||
| Molar Mass | 443.88 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Samuvel DJ, et al. AKP-11 - A Novel S1P1 Agonist with Favorable Safety Profile Attenuates Experimental Autoimmune Encephalomyelitis in Rat Model of Multiple Sclerosis. PLoS One. 2015 Oct 29;10(10):e0141781. |