JTE 013

Pricing Availability Delivery Time Qty
Cat.No. 2392 - JTE 013 | C17H19N7OCl2 | CAS No. 547756-93-4
Description: S1P2 receptor antagonist
Chemical Name: 1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(3,5-dichloro-4-pyridinyl)-semicarbazide
Purity: ≥98% (HPLC)
Datasheet
Citations (18)
Literature

Biological Activity

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.

Compound Libraries

JTE 013 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 408.29
Formula C17H19N7OCl2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 547756-93-4
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.83 100
ethanol 40.83 100

Preparing Stock Solutions

The following data is based on the product molecular weight 408.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: S1P2 receptor antagonists Receptors EDG5 Sphingosine-1-Phosphate JTE013 Sphingosine-1-phosphate Receptors

18 Citations for JTE 013

Citations are publications that use Tocris products. Selected citations for JTE 013 include:

Wirrig et al (2016) Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells Biochemical Pharmacology 115 43 PMID: 27402344

Kellner et al (2016) Nogo-A controls structural plasticity at dendritic spines by rapidly modulating actin dynamics. Hippocampus 6 816 PMID: 26748478

Gu et al (2015) Defective apical extrusion signaling contributes to aggressive tumor hallmarks. Elife 4 e04069 PMID: 25621765

Durham et al (2015) Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy? Arthritis Rheum 56 3441 PMID: 26030100

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

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

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

Stradner et al (2013) Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes. J Urol 65 2113 PMID: 23666803

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

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

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

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

Li et al (2009) S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor. J Biol Chem 181 1347 PMID: 19157443

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

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


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