Home GPCR & G Protein S1P Receptor antagonist JTE 013 For research use only.

JTE 013

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

JTE 013 Chemical Structure

JTE 013 Chemical Structure

CAS: 383150-41-2

Selleck's JTE 013 has been cited by 8 publications

Purity & Quality Control

Batch: S718201 DMSO] 81 mg/mL] false] Ethanol] 34 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

JTE 013 Related Products

Signaling Pathway

S1P Receptor Signaling Pathways

S1P Receptor Signaling Pathway

Choose Selective S1P Receptor Inhibitors

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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot SK1 / SK2 22095950
In Vivo
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].
Animal Research Animal Models Mice(C57BL/6×129Sv genetic background)
Dosages 1.2 mg/kg
Administration i.p

Chemical Information & Solubility

Molecular Weight 408.29 Formula

C17H19Cl2N7O
CAS No. 383150-41-2 SDF Download JTE 013 SDF
Smiles CC1=NN(C2=C1C(=CC(=N2)NNC(=O)NC3=CC(=NC(=C3)Cl)Cl)C(C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (198.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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