The sphingosine 1-phosphate (S1P) receptor S1P3 has roles in vasodilation, epithelial barrier function, cardioprotection, fibrosis, immunity, and inflammation. CYM 5541 is a selective, allosteric agonist of S1P3 (EC50 = 72-132 nM). It less effectively activates S1P1 (EC50 = 28-38 μM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.
