JTE-013|JTE013|S1P2 antagonist|cas 944547-46-0

JTE-013|JTE013|S1P2 antagonist|cas 944547-46-0

DC Chemicals, Website: www.dcchemicals.com

Product Name: JTE-013|Cas Number: 383150-41-2| Catalog Number: DC10607|Other Nmaes: JTE-013,JTE 013,JTE013

JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.

JTE-013 reverses the inhibitory effects of S1P2 signaling on cell migration of vascular ECs and smooth muscle cells. It 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.JTE-013 inhibition of S1P2 significantly inhibits microvascular permeability in an in vivo animal model. JTE-013 modulates the responses of brain endothelium by inhibiting cerebrovascular permeability, the development of intracerebral heamorrhage, and neurovascular injury in an experimental model of stroke. JTE-013 reduced mast cell activation, airway infiltration, and the serum levels of histamine and several cytokines in vitro and in vivo studies. In a murine model, JTE-013 suppresses streptozotocin-induced blood glucose increases, pancreatic b cell apoptosis, and the incidence of diabetes. In a New Zealand obese diabetic mouse model under high-fat diet conditions, it protected pancreatic b cells. Treatment with JTE-013 also reduces plasma levels of IL-1b and IL-18 (endotoxin-induced inflammatory cytokines) in ApoE−/− mice and S1P2 gene deficiency reduces atherosclerosis. The compound offers a novel means of treating inflammatory disorders, such as, atherosclerosis and sepsis.