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J4080

Sigma-Aldrich

JTE-013

≥98% (HPLC)

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

color

white to off-white

solubility

DMSO: ≥20 mg/mL

storage temp.

2-8°C

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

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 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_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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