JTE-013 (JTE013) is a potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 17 nM and 22 nM for human and rat S1P2, respectively.
JTE-013 does not affect S1P binding to S1P3 and S1P1 at 10 uM.
JTE-013 inhibits not only S1P-induced vasoconstriction, but also KCl-, U46619- and endothelin-1-induced constriction in vivo.
JTE-013 abrogates S1P induced inhibition and activation, respectively, of Rac and RhoA in B16 cells.
