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Submit ReviewJTE 013 is a sphingosine-1-phosphate (S1P) receptor antagonist, highly selective for S1P2 (EDG-5). Inhibits S1P binding to human S1P2 receptors with an IC50 value of 17.6 nM. At concentrations up to 10 μM, displays 4.2% inhibition of S1P3 and does not antagonize S1P1. Enhances S1P-induced angiogenesis in vivo.
JTE 013 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 408.29 |
公式 | C17H19N7OCl2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 383150-41-2 |
PubChem ID | 10223146 |
InChI Key | RNSLRQNDXRSASX-UHFFFAOYSA-N |
Smiles | CC(C)C1=C2C(C)=NN(C)C2=NC(NNC(=O)NC2=CC(Cl)=NC(Cl)=C2)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.83 | 100 | |
ethanol | 40.83 | 100 |
以下数据基于产品分子量 408.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.45 mL | 12.25 mL | 24.49 mL |
5 mM | 0.49 mL | 2.45 mL | 4.9 mL |
10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Ohmori et al (2003) Spingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc.Res. 58 170 PMID: 12667959
Parrill et al (2004) Sphingosine 1-phosphate and lysophosphatidic acid receptors: agonist and antagonist binding and progress toward development of receptor-specific ligands. Semin.Cell.Dev.Biol. 15 467 PMID: 15271292
Inoki et al (2006) Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochem.Biophys.Res.Comm. 346 293
If you know of a relevant reference for JTE 013, please let us know.
关键词: JTE 013, JTE 013 supplier, S1P2, receptor, antagonists, Receptors, EDG5, Sphingosine-1-Phosphate, JTE013, Sphingosine-1-phosphate, 2392, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 JTE 013 的部分引用包括:
Chumanevich et al (2016) Sphingosine-1-Phosphate/Sphingosine-1-Phosphate Receptor 2 Axis Can Promote Mouse and Human Primary Mast Cell Angiogenic Potential through Upregulation of Vascular Endothelial Growth Factor-A and Matrix Metalloproteinase-2. Mediators Inflamm 2016 1503206 PMID: 26884643
Szczepaniak et al (2010) S1P2 receptor-dependent Rho-kinase activation mediates vasoconstriction in the murine pulmonary circulation induced by sphingosine 1-phosphate. Am J Physiol Lung Cell Mol Physiol 299 L137 PMID: 20435688
Long et al (2010) Sphingosine 1-phosphate receptor 4 uses HER2 (ERBB2) to regulate extracellular signal regulated kinase-1/2 in MDA-MB-453 breast cancer cells. J Biol Chem 285 35957 PMID: 20837468
Kellner et al (2016) Nogo-A controls structural plasticity at dendritic spines by rapidly modulating actin dynamics. Hippocampus 6 816 PMID: 26748478
Durham et al (2015) Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy? Arthritis Rheum 56 3441 PMID: 26030100
Zhang et al (2010) Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules. Cardiovasc Res 299 H1494 PMID: 20729401
Frias et al (2010) Native and reconstituted HDL protect cardiomyocytes from doxorubicin-induced apoptosis. Mol Cancer Res 85 118 PMID: 19700468
Matsushima-Nishiwaki et al (2018) Sphingosine 1-phosphate (S1P) reduces hepatocyte growth factor-induced migration of hepatocellular carcinoma cells via S1P receptor 2 PLoS One 13 e0209050 PMID: 30543684
Wirrig et al (2016) Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells Biochemical Pharmacology 115 43 PMID: 27402344
Shen et al (2014) Sphingosine 1-phosphate (S1P) promotes mitochondrial biogenesis in Hep G2 cells by activating Peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α). Cell Stress Chaperones 19 541 PMID: 24293320
Gu et al (2015) Defective apical extrusion signaling contributes to aggressive tumor hallmarks. Elife 4 e04069 PMID: 25621765
Fernández-Pisonero et al (2014) Synergy between sphingosine 1-phosphate and lipopolysaccharide signaling promotes an inflammatory, angiogenic and osteogenic response in human aortic valve interstitial cells. Am J Physiol Heart Circ Physiol 9 e109081 PMID: 25275309
Quint et al (2013) Sphingosine 1-phosphate (S1P) receptors 1 and 2 coordinately induce mesenchymal cell migration through S1P activation of complementary kinase pathways. PLoS One 288 5398 PMID: 23300082
Stradner et al (2013) Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes. J Urol 65 2113 PMID: 23666803
Green et al (2011) The sphingosine 1-phosphate receptor S1P2 maintains the homeostasis of germinal center B cells and promotes niche confinement. Nat Immunol 12 672 PMID: 21642988
Li et al (2008) Induction of antiproliferative connective tissue growth factor expression in Wilms' tumor cells by sphingosine-1-phosphate receptor 2. J Clin Endocrinol Metab 6 1649 PMID: 18922980
Li et al (2009) S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor. J Biol Chem 181 1347 PMID: 19157443
Beckham et al (2013) Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling. Oncogenesis 2 e49 PMID: 23732709
Beckham et al (2013) Acid ceramidase promotes nuclear export of PTEN through sphingosine 1-phosphate mediated Akt signaling. PLoS One 8 e76593 PMID: 24098536
Miller et al (2008) Sphingosine kinases and sphingosine-1-phosphate are critical for transforming growth factor beta-induced extracellular signal-regulated kinase 1 and 2 activation and promotion of migration and invasion of esophageal cancer cells. Mol Cell Biol 28 4142 PMID: 18426913
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