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Description: JTE 013 is a novel potent and selective S1P2 (sphingosine-1-phosphate 2) antagonist with IC50 of 17.6 nM. It binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, and with IC50 values > 10 uM for human S1P1 and S1P3. It reverses the inhibitory effects of S1P2 signaling on cell migration of vascular ECs and smooth muscle cells. It also regulates endothelial tight junctions and barrier function in vitro. Blockage of S1P2 signaling by JTE-013 significantly enhances the effects of S1P on the increase of TEER, an in vitro measurement of endothelial integrity, as well as the formation of TJs in senescent ECs.
References: Am J Physiol Heart Circ Physiol. 2009 Jan; 296(1):H33-42.
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