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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 383150-41-2 Chemical Structure| 383150-41-2

Structure of JTE-013
CAS No.: 383150-41-2

Chemical Structure| 383150-41-2

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JTE 013 is a potent, selective S1P2 receptor antagonist with IC50 value of 17.6 nM.

4.5 *For Research Use Only !

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Product Details of JTE-013

CAS No. :383150-41-2
Formula : C17H19Cl2N7O
M.W : 408.29
SMILES Code : CC(C1=C2C(N(C)N=C2C)=NC(NNC(NC3=CC(Cl)=NC(Cl)=C3)=O)=C1)C
MDL No. :MFCD09878275
InChI Key :RNSLRQNDXRSASX-UHFFFAOYSA-N
Pubchem ID :10223146

Safety of JTE-013

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Related Pathways of JTE-013

GPCR

Isoform Comparison

Biological Activity

In Vitro:

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. Cell Rep. 2020 Jun 30;31(13):107828
HT-29 cells 10 μM 24 hours JTE-013 effectively inhibited S1P-induced S1PR2 internalization, thereby reversing 5-FU resistance. Acta Pharmacol Sin. 2021 Mar;42(3):460-469
HCT116 cells 10 μM 24 hours JTE-013 effectively inhibited S1P-induced S1PR2 internalization, thereby reversing 5-FU resistance. Acta Pharmacol Sin. 2021 Mar;42(3):460-469
RAW264.7 cells 10 µM 4 hours 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

In Vivo:

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

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.25mL

2.45mL

1.22mL

24.49mL

4.90mL

2.45mL

References

 

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