JTE 013

Catalog No.S7182 Batch:S718201

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Technical Data

Formula

C17H19Cl2N7O
Molecular Weight 408.29 CAS No. 383150-41-2
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)
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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].
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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[4]
  • Animal Models

    Mice(C57BL/6×129Sv genetic background)

  • Dosages

    1.2 mg/kg

  • Administration

    i.p

Selleck's JTE 013 has been cited by 8 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.