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JTE-013

产品编号: DC10607 Featured
JTE-013
结构式
383150-41-2
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中国地区超过5000个高品质化合物库存
应用领域
JTE-013 是一种有效且选择性的 S1P2 (鞘氨醇1-磷酸2) 拮抗剂。JTE-013 抑制放射性标记的 S1P 与人和大鼠 S1P2 的特异性结合，IC50 分别为 17 nM 和 22 nM。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 383150-41-2
名称:
别名: JTE-013,JTE 013,JTE013
SMILES: ClC1C=C(NC(NNC2N=C3N(C)N=C(C)C3=C(C(C)C)C=2)=O)C=C(Cl)N=1
分子式: C17H19Cl2N7O
分子量: 408.29
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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