AKP-11

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 healthy control animals, when administered at a dose of 1.3 mg/kg.

WARNING This product is not for human or veterinary use.

1. Gill, G.S., and Grobelny, D.W. S1P receptors modulators and their use thereof. (2009).

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).