JTE 013 is a potent, selective S1P2 receptor antagonist with IC50 value of 17.6 nM.
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JTE-013 is recognized as a potent and selective antagonist of S1P2. It effectively blocks the binding of radiolabeled S1P to S1P2 receptors in both humans and rats, with IC50 values of 17 nM and 22 nM, respectively. When applied at concentrations ranging from 50 to 200 μM for 1 to 3 days, JTE-013 leads to a reduction in cell viability[1]. At dosages between 10 and 1000 nM over 30 minutes, JTE-013 counteracts the Akt inhibition induced by S1P and impedes the activation of ERK by S1P. JTE-013 shows a modest 4.2% inhibition of S1P3 and does not act as an antagonist to S1P1 at concentrations up to 10 μM. In SK-N-AS cells, exposure to 50, 100, 150, and 200 μM of JTE-013 for 1-3 days results in decreased cell viability, while 10, 100, and 1000 nM concentrations over 30 minutes reverse S1P-induced Akt inhibition and inhibit S1P-induced ERK activation[1].
JTE-013 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human brain microvascular endothelial cells (hBMVEC)
0.1 μM or 1 μM
24 hours
To study the role of S1PR2 in brain endothelial cell responses to ischemic/reperfusion injury. Results showed that JTE013 inhibited TNF-α-induced MMP-9 activity.
Nat Commun. 2015 Aug 5;6:7893
Mouse brain endothelial cell line bEnd.3
1 μM
24 hours
To evaluate the role of S1PR2 in brain endothelial cell permeability and MMP-9 activation. Results showed that JTE013 significantly inhibited TNF-α-induced MMP-9 activity.
Nat Commun. 2015 Aug 5;6:7893
266-6 cells
10 µM
4 hours
Inhibited TCA-induced NF-κB activation
Cell Commun Signal. 2022 Oct 13;20(1):157
mouse large cholangiocytes (MLE)
10 μM
24 hours
inhibited TCA- and S1P-induced cell invasion
Hepatology. 2017 Jun;65(6):2005-2018
mouse large cholangiocytes (MLE)
10 μM
30 minutes
inhibited TCA- and S1P-induced AKT and ERK1/2 phosphorylation
Hepatology. 2017 Jun;65(6):2005-2018
alveolar type II cells
10 μM
14 days
To evaluate the effect of JTE-013 on the differentiation of alveolar type II cells in 3D culture. Results showed a significant reduction in the percentage of HopX+ cells in JTE-013-treated organoids.
Cell Rep. 2020 Jun 30;31(13):107828
alveolar type II cells
10 μM
3 days
To evaluate the effect of JTE-013 on the differentiation of alveolar type II cells to type I cells. Results showed a significant reduction in the percentage of Ager+ cells in JTE-013-treated cells.
Inhibited TCA-induced NF-κB activation and macrophage migration
Cell Commun Signal. 2022 Oct 13;20(1):157
bone marrow-derived dendritic cells (BMDCs)
1-30μM
24 hours
suppressed IL-4-induced CCL17 and CCL22 expression in a dose-dependent manner
Acta Pharmacol Sin. 2020 Nov;41(11):1487-1496
A10 VSMCs
1 μM
30 minutes
JTE-013, as an S1PR2 antagonist, was used to block the inhibitory effect of MYDGF on VSMC phenotypic switching via the S1PR2-Rho-ROCK-F/G-actin-MRTF-A signaling pathway. Results showed that JTE-013 pretreatment partially abolished the inhibitory effects of MYDGF on PDGF-BB-induced VSMC proliferation, migration, and dedifferentiation.
Acta Pharmacol Sin. 2024 Jan;45(1):98-111
JTE-013 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
DDC-induced cholestatic liver fibrosis model
Intraperitoneal injection
10 mg/kg
Three times per week for 4 weeks
JTE-013 significantly attenuated liver injury and fibrogenesis in DDC-induced liver fibrosis model.
Clin Mol Hepatol. 2023 Apr;29(2):465-481
ICR mice
DDC-induced liver fibrosis model
Intraperitoneal injection
10 mg/kg
Three times per week for 4 weeks
JTE-013 significantly attenuated liver histopathological injury, collagen accumulation, and the expression of fibrogenesis-associated genes in mice fed a DDC diet
Clin Mol Hepatol. 2023 Apr;29(2):465-481
Mice
PA-induced lung injury model
Intratracheal injection
1 mg/kg
Single injection at 72 hours post-PA injury
To evaluate the effect of JTE-013 on the differentiation of alveolar type II cells to type I cells in vivo. Results showed significantly fewer Tomato+ squamous cells in JTE-013-treated lungs.
Cell Rep. 2020 Jun 30;31(13):107828
ICR mice
Acute pancreatitis model
Intraperitoneal injection
10 mg/kg
Once, 1 hour before the first caerulein injection
Alleviated pancreatic injury and inflammatory response
Cell Commun Signal. 2022 Oct 13;20(1):157
Balb/c mice
DNCB-induced atopic dermatitis model
Intraperitoneal injection
3 mg/kg
From D19 to D49, administered 30 min before each DNCB challenge
Significantly suppressed DNCB-induced atopic responses in ears and lymph nodes, reduced lymph node size, levels of inflammatory cytokines, and expression of chemokines CCL17 and CCL22
Acta Pharmacol Sin. 2020 Nov;41(11):1487-1496
Balb/c mice
OVA-induced asthma model
Intraperitoneal injection
3 mg/kg
Administered 30 min before OVA sensitization, before OVA challenge, or before both events
To evaluate the role of JTE-013 in an OVA-induced asthma model. Results showed that JTE-013 significantly inhibited eosinophil accumulation and elevated Th2 cytokine levels (IL-4, IL-5, and IL-13) in BALF, and alleviated lung inflammation and mucus production.
Br J Pharmacol. 2019 Apr;176(7):938-949
Mice
Transient middle cerebral artery occlusion model (tMCAO)
Oral gavage
30 mg/kg
Single dose administered 10 minutes after reperfusion
To evaluate the effect of S1PR2 on cerebrovascular integrity in experimental stroke. Results showed that JTE013 significantly reduced brain infarct and edema ratios and improved neurological scores.
Nat Commun. 2015 Aug 5;6:7893
JTE-013 动物研究
Animal study
Through oral administration of JTE-013 at a dosage of 30 mg/kg daily for a span of 14 days, there is a notable decrease in both the dimensions and mass of tumors[3].
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