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^[1][2][3][4]. 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]. 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].