JTE 013

Catalog No.S7182

JTE 013 Chemical Structure

Molecular Weight(MW): 408.29

JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.

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Biological Activity

Description JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
Targets
S1PR2(human) [1]
(in CHO cells)
S1PR2(rat) [1]
(in CHO cells)
17 nM 22 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].

Assay
Methods Test Index PMID
Western blot
SK1 / SK2; 

PubMed: 22095950     


Renal sphingosine kinase protein expression in HK-2 cells treated with vehicle or JTE-013 for 6 hours.

22095950
Growth inhibition assay
Cell viability; 

PubMed: 26105954     


Effect of JTE-013 and AB1 on cell viability in SK-N-AS cells. Cells were plated in 96-well plates. The next day, they were treated with JTE-013 and AB1 for 1–3 days, followed by the MTT assay. The percentage of cell viability was calculated relative to the dimethylsulfoxide control. Data are the means ± S.E. of triplicates. #P < 0.05; ##P < 0.01 versus corresponding JTE-013–treated cells, using the two-tailed homoscedastic t test. Con, concentration.

26105954
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].

Protocol

Cell Research:

[1]

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  • Cell lines: Human umbilical vein endothelial cells (HUVECs)
  • Concentrations: 0.01, 0.1, 1 μM
  • Incubation Time: 10 min
  • Method:

    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.


    (Only for Reference)
Animal Research:

[4]

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  • Animal Models: Mice(C57BL/6×129Sv genetic background)
  • Formulation: --
  • Dosages: 1.2 mg/kg
  • Administration: i.p
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (198.38 mM)
Ethanol 34 mg/mL (83.27 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG 300+ 5% Tween80 + ddH2O
For best results, use promptly after mixing.
6.25mg/mL

* 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.

Chemical Information

Molecular Weight 408.29
Formula

C17H19Cl2N7O

CAS No. 383150-41-2
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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S1P Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID