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. |2. 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). |