1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  2. Cannabinoid Receptor TRP Channel Interleukin Related ANGPTL VEGFR
  3. JTE-907

JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis.

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JTE-907

JTE-907 Chemical Structure

CAS No. : 282089-49-0

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JTE-907 is a selective and orally active cannabinoid CB2 receptor inverse agonist and exerts anti-inflammatory effects. JTE-907 upregulates IL-6, MCP-1, IL-1β, VEGF, ANGPTL4, and TRPV1 in mature adipocytes. JTE-907 downregulates CB1, MCP-1, and IL-1β in preadipocytes. JTE-907 inhibits ear swelling in mice. JTE-907 reverses the protective effects of CB2 agonists and Anandamide (HY-10863) against cytokine-evoked colonic mucosal damage. JTE-907 can be used for the research of allergic dermatitis, obesity, and colitis[1][2][3][4].

IC50 & Target[1][2]

CB2

 

CB1

 

IL-6

 

IL-1β

 

TRPV1

 

ANGPTL4

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
644 nM
Compound: JTE-907
Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay
Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay
[PMID: 24445310]
In Vitro

JTE-907 (1-10 μM; 4-20 h) upregulates pro-inflammatory and angiogenic gene expression and IL-6 secretion in mature human subcutaneous adipocytes via CB1 and TRPV1 receptors[2].
JTE-907 (10 μM; 20 h) downregulates CB1, MCP-1, and IL-1β gene expression in human subcutaneous preadipocytes[2].
JTE-907 (0.1 μM; 20 h) reverses the CB2 receptor-mediated protective effects of Anandamide (HY-10863) and JWH-015 against cytokine-induced colitis-like damage in healthy human colonic mucosal explants, including restoring crypt damage, luminal epithelial damage, and lamina propria lymphocyte density to levels comparable to cytokine-only treatment[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JTE-907 (0.01-10 mg/kg; p.o.; single dose 1 h pre-2-AG-E exposure) inhibits both early and late 2-AG-E-induced cutaneous ear swelling in female BALB/c mice, with partial dose-dependent suppression of the late response at lower doses[1].
JTE-907 (0.01-10 mg/kg; p.o.; single dose 1 h pre-arachidonic acid exposure) does not inhibit arachidonic acid-induced cutaneous ear swelling in female BALB/c mice[1].
JTE-907 (0.1-10 mg/kg; p.o.; once daily for 6 days plus two doses around the 4th DNFB exposure) significantly suppresses DNFB-induced allergic dermatitis ear swelling in female BALB/c mice without inducing systemic immunosuppression-related changes to spleen or thymus weight[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

438.47

Formula

C24H26N2O6

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC2=C(NC1=O)C(OCCCCC)=C(OC)C=C2)NCC3=CC=C(OCO4)C4=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (285.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2807 mL 11.4033 mL 22.8066 mL
5 mM 0.4561 mL 2.2807 mL 4.5613 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2807 mL 11.4033 mL 22.8066 mL 57.0164 mL
5 mM 0.4561 mL 2.2807 mL 4.5613 mL 11.4033 mL
10 mM 0.2281 mL 1.1403 mL 2.2807 mL 5.7016 mL
15 mM 0.1520 mL 0.7602 mL 1.5204 mL 3.8011 mL
20 mM 0.1140 mL 0.5702 mL 1.1403 mL 2.8508 mL
25 mM 0.0912 mL 0.4561 mL 0.9123 mL 2.2807 mL
30 mM 0.0760 mL 0.3801 mL 0.7602 mL 1.9005 mL
40 mM 0.0570 mL 0.2851 mL 0.5702 mL 1.4254 mL
50 mM 0.0456 mL 0.2281 mL 0.4561 mL 1.1403 mL
60 mM 0.0380 mL 0.1901 mL 0.3801 mL 0.9503 mL
80 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
100 mM 0.0228 mL 0.1140 mL 0.2281 mL 0.5702 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JTE-907
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HY-103325
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