J4080
JTE-013
≥98% (HPLC), sphingosine 1-phosphate (S1P) receptor antagonist, powder
别名:
1-[1,3-二甲基-4-（2-甲基乙基）-1H-吡唑并 [3,4-b] 吡啶-6-基]-4-（2,6-二氯-4-吡啶）-氨基脲
Product Name
JTE-013, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to off-white
溶解性
DMSO: ≥20 mg/mL
储存温度
2-8°C
SMILES字符串
Clc1nc(cc(c1)NC(=O)NNc2nc3[n](nc(c3c(c2)C(C)C)C)C)Cl
InChI
1S/C17H19Cl2N7O/c1-8(2)11-7-14(22-16-15(11)9(3)25-26(16)4)23-24-17(27)20-10-5-12(18)21-13(19)6-10/h5-8H,1-4H3,(H,22,23)(H2,20,21,24,27)
InChI key
RNSLRQNDXRSASX-UHFFFAOYSA-N
相关类别
应用
JTE-013 已用于 体外 血液-脑屏障 (BBB) 和血-肿瘤屏障 (BTB) 试验。
生化/生理作用
JTE-013 是一种选择性 1-磷酸鞘氨醇 (S1P) 受体拮抗剂。
JTE-013 是一种选择性 1-磷酸鞘氨醇 (S1P) 受体拮抗剂。JTE-013 对 S1P2 (EDG-5) 具有高度选择性。抑制 S1P 与人 S1P2 受体结合，IC50 值为 17.6 nM。在浓度高达 10 mM 时，JTE-013 对 S1P3 的抑制率为 4.2%，不拮抗 S1P1
JTE-013 能增强小直径感觉神经元的兴奋性。它具有抑制 1-磷酸鞘氨醇 (S1P) 介导的细胞迁移的能力。
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Haowen Ye et al.
Frontiers in pharmacology, 12, 721200-721200 (2021-08-21)
Aims: To explore the role of the Sphingosine 1-Phosphate (S1P)/Receptor2 (S1PR2) pathway in thrombin-induced hyperpermeability (TIP) and to test whether bivalirudin can reverse TIP via the S1P-S1PRs pathway. Methods and Results: Using western blot, we demonstrated that Human umbilical vein
Sphingosine 1-phosphate receptor 2 antagonist JTE-013 increases the excitability of sensory neurons independently of the receptor
Li C, et al.
Journal of Neurophysiology, 108(5), 1473-1483 (2012)
K Liu et al.
Andrology, 8(2), 497-508 (2019-10-15)
Erectile dysfunction (ED) is a common complication in patients with diabetes mellitus (DM) that severely affects the patients' quality of life. However, the effectiveness of oral phosphodiesterase type 5 inhibitors in these patients is poor. Sphingosine-1-phosphate (S1P) and S1P receptor
Reactive astrocytic S1P3 signaling modulates the blood-tumor barrier in brain metastases
Gril B, et al.
Nature Communications, 9(1), 2705-2705 (2018)
Xiaofei Sun et al.
Biochemical and biophysical research communications, 527(1), 131-137 (2020-05-25)
To investigate the expression of Nogo-A in dorsal root ganglion (DRG) in rats with cauda equina injury and the therapeutic effects of blocking Nogo-A and its receptor. Fifty-eight male Sprague-Dawley rats were divided randomly into either the sham operation group
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