A CB2 receptor inverse agonist
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JTE-907

Item No. 10009857

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1,3-benzodioxol-5-ylmethyl)-1,2-dihydro-7-methoxy-2-oxo-8-(pentyloxy)-3-quinolinecarboxamide
CAS Number
282089-49-0
Molecular Formula
C24H26N2O6
Formula Weight
438.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16.6 mg/mlDMF:PBS (pH 7.2) (1:2): 0.2 mg/mlDMSO: 0.16 mg/mlMethanol: 1 mg/ml
λmax
222, 264, 331 nm
SMILES
O=C1NC2=C(OCCCCC)C(OC)=CC=C2C=C1C(NCC3=CC=C(OCO4)C4=C3)=O
InChi Code
InChI=1S/C24H26N2O6/c1-3-4-5-10-30-22-19(29-2)9-7-16-12-17(24(28)26-21(16)22)23(27)25-13-15-6-8-18-20(11-15)32-14-31-18/h6-9,11-12H,3-5,10,13-14H2,1-2H3,(H,25,27)(H,26,28)
InChi Key
GRAJFFFXJYFVOC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    JTE-907 is a cannabinoid 2 (CB2) receptor inverse agonist.1 It is selective for CB2 over CB1 receptors (Kis = 35.9 and 2,370 nM, respectively, for the human receptors). JTE-907 increases forskolin-induced cAMP production in CHO cells expressing human or mouse CB2 receptors in a concentration-dependent manner. It promotes the differentiation of isolated mouse splenic CD4+ T cells into regulatory T cells (Tregs) when used at a concentration of 100 nM and decreases disease severity in a mouse model of inflammatory bowel disease (IBD) induced by dinitrobenzene sulfonic acid (DNBS).2 JTE-907 (1 and 10 mg/kg) inhibits spontaneous scratching in a mouse model of chronic dermatitis, as well as reduces carrageenan-induced paw edema in mice (ED50 = 0.05 mg/kg).3,1 Bilateral injection of JTE-907 (25 pmol/animal) into the anterior bed nucleus of the stria terminalis decreases the percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiety-like behavior.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Iwamura, H., Suzuki, H., Ueda, Y., et al. In vitro and in vivo pharmacological characterization of JTE-907, a novel selection ligand for cannabinoid CB2 receptor. J. Pharmacol. Exp. Ther. 296(2), 420-425 (2001).

    2. Gentili, M., Ronchetti, S., Ricci, E., et al. Selective CB2 inverse agonist JTE907 drives T cell differentiation towards a Treg cell phenotype and ameliorates inflammation in a mouse model of inflammatory bowel disease. Pharmacol. Res. 141, 21-31 (2019).

    3. Maekawa, T., Nojima, H., Kuraishi, Y., et al. The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. Euro. J. Pharmacol. 542(1-3), 179-183 (2006).

    4. Gomes-de-Souza, L., Bianchi, P.C., Costa-Ferreira, W., et al. CB1 and CB2 receptors in the bed nucleus of the stria terminalis differently modulate anxiety-like behaviors in rats. Prog. Neuropsychopharmacol. Biol. Psychiatry 110, 110284 (2021).