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J4080

JTE-013

≥98% (HPLC), sphingosine 1-phosphate (S1P) receptor antagonist, powder

Synonym(s):

1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(2,6-dichloro-4-pyridinyl)-semicarbazide

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About This Item

Empirical Formula (Hill Notation):
C17H19N7OCl2
CAS Number:
383150-41-2
Molecular Weight:
408.29
UNSPSC Code:
12352211
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Product Name

JTE-013, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to off-white

solubility

DMSO: ≥20 mg/mL

storage temp.

2-8°C

SMILES string

Clc1nc(cc(c1)NC(=O)NNc2nc3[n](nc(c3c(c2)C(C)C)C)C)Cl

InChI

1S/C17H19Cl2N7O/c1-8(2)11-7-14(22-16-15(11)9(3)25-26(16)4)23-24-17(27)20-10-5-12(18)21-13(19)6-10/h5-8H,1-4H3,(H,22,23)(H2,20,21,24,27)

InChI key

RNSLRQNDXRSASX-UHFFFAOYSA-N

Related Categories

Application

JTE-013 has been used in in vitro blood−brain barrier (BBB) and blood−tumor barrier (BTB) assays.

Biochem/physiol Actions

JTE-013 can enhance the excitability of small-diameter sensory neurons. It has the ability to repress sphingosine 1-phosphate (S1P)-mediated cellular migration.
JTE-013 is a selective sphingosine 1-phosphate (S1P) receptor antagonist.
JTE-013 is a selective sphingosine 1-phosphate (S1P) receptor antagonist. JTE-013 is highly selective for S1P2 (EDG-5). It inhibits S1P binding to human S1P2 receptors with an IC50 value of 17.6 nM. At concentrations up to 10 mM, JTE-013 displays 4.2% inhibition of S1P3 and does not antagonise S1P1.

Features and Benefits

This compound is featured on the Lysophospholipid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000202713
0000202713
0000144772
0000144772
0000144773

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Sphingosine 1-phosphate receptor 2 antagonist JTE-013 increases the excitability of sensory neurons independently of the receptor
Li C, et al.
Journal of Neurophysiology, 108(5), 1473-1483 (2012)
K Liu et al.
Andrology, 8(2), 497-508 (2019-10-15)
Erectile dysfunction (ED) is a common complication in patients with diabetes mellitus (DM) that severely affects the patients' quality of life. However, the effectiveness of oral phosphodiesterase type 5 inhibitors in these patients is poor. Sphingosine-1-phosphate (S1P) and S1P receptor
Reactive astrocytic S1P3 signaling modulates the blood-tumor barrier in brain metastases
Gril B, et al.
Nature Communications, 9(1), 2705-2705 (2018)
Xiaofei Sun et al.
Biochemical and biophysical research communications, 527(1), 131-137 (2020-05-25)
To investigate the expression of Nogo-A in dorsal root ganglion (DRG) in rats with cauda equina injury and the therapeutic effects of blocking Nogo-A and its receptor. Fifty-eight male Sprague-Dawley rats were divided randomly into either the sham operation group
Haowen Ye et al.
Frontiers in pharmacology, 12, 721200-721200 (2021-08-21)
Aims: To explore the role of the Sphingosine 1-Phosphate (S1P)/Receptor2 (S1PR2) pathway in thrombin-induced hyperpermeability (TIP) and to test whether bivalirudin can reverse TIP via the S1P-S1PRs pathway. Methods and Results: Using western blot, we demonstrated that Human umbilical vein
View All Related Papers

Global Trade Item Number

SKUGTIN
J4080-25MG04061833219270
J4080-5MG04061833219287

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