JTE 013

製品コードS7182 バッチS718201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H19Cl2N7O
分子量 408.29 CAS No. 383150-41-2
Solubility (25°C)* 体外 DMSO 81 mg/mL (198.38 mM)
Ethanol 34 mg/mL (83.27 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
6.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 125 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
in vitro 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[2].
in vivo JTE-013 inhibition of S1P2 significantly inhibits microvascular permeability in an in vivo animal model[2]. 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[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human umbilical vein endothelial cells (HUVECs)
濃度 0.01, 0.1, 1 μM
反応時間 10 min
実験の流れ

HUVECs preincubated with various concentrations of JTE-013 for 10 min are allowed to migrate for 4 h toward the lower chamber where the indicated concentrations of Sph-1-P are placed. The migrated cells on the lower side of the filter are fixed, stained, and counted.
動物実験 動物モデル Mice(C57BL/6×129Sv genetic background)
投薬量 1.2 mg/kg
投与方法 i.p

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Comprehensive metabolomics expands precision medicine for triple-negative breast cancer [ Cell Res, 2022, 10.1038/s41422-022-00614-0] PubMed: 35105939
RTN4/Nogo-A-S1PR2 negatively regulates angiogenesis and secondary neural repair through enhancing vascular autophagy in the thalamus after cerebral cortical infarction [ Autophagy, 2022, 1-20] PubMed: 35263212
CRH/CRHR1 modulates cerebrovascular endothelial cell permeability in association with S1PR2 and S1PR3 under oxidative stress [ Vascul Pharmacol, 2021, S1537-1891(21)00113-0] PubMed: 34781017
MAPK activity dynamics regulate non-cell autonomous effects of oncogene expression [ Elife, 2020, 9e60541] PubMed: 32940599
Resveratrol Inhibits Lipopolysaccharide-Induced Extracellular Matrix Accumulation and Inflammation in Rat Glomerular Mesangial Cells by SphK1/S1P2/NF-κB Pathway [ Diabetes Metab Syndr Obes, 2020, 13:4495-4505] PubMed: 33262625
S1PR2 Knockdown Promotes Migration and Invasion in Multiple Myeloma Cells via NF-κB Activation [ Cancer Manag Res, 2020, 12:7857-7865] PubMed: 32922084
S100A4+ Macrophages Are Necessary for Pulmonary Fibrosis by Activating Lung Fibroblasts [ Front Immunol, 2018, 9:1776] PubMed: 30127784
Changes of Foxo3a in PBMCs and its associations with stress hyperglycemia in acute obstructive suppurative cholangitis patients [ Oncotarget, 2017, 8(44):76783-76796] PubMed: 29100348

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。