ML248 (CYM50308) is a potent and selective S1P4 receptor agonist with EC50 of 37.7 nM-79.1 nM.
ML248 (CYM50308) is inactive as an agonist against other members of the receptor family, with EC50s >25 μM against S1P1, S1P2, and S1P3 receptors, and an EC50 of 2.1 μM against the S1P5 receptor.
ML248 (CYM50308) is inhibited by an S1P4 receptor-selective antagonist, inactive for agonism in the presence of >3.7 nM selective antagonist and is nontoxic to U2OS cells.
ML248 (CYM50308) increased expression of the chemokine receptor CXCR4 in compound treated CD8+ T lymphocytes.
