TRPA1 Agonist

Nepetalactone is a TRPA1 agonist (EC₅₀ = 172.5-698.4 μM) and antibacterial agent that can be present in the essential oils of Nepeta crispa and Nepeta rtanjensis. Nepetalactone activates TRPA1 orthologs through a conserved cysteine-rich CVT motif, triggering calcium influx, thereby driving pest aversion through PKCα and attracting predators through CaMKII, and can suppress pests in the field. Nepetalactone inhibits bacterial and fungal biofilms and produces additive interactions with 1,5,9-eDLA and RA. Nepetalactone induces ROS production in macrophages. Nepetalactone can be used in research related to foodborne infections, pest control, and bacterial and fungal infections.

Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC₅₀=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.

TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, with EC₅₀ values of 50.05 μM and 314.04 μM for human and mouse TRPA1, respectively. TRPA1 agonist-3 does not activate hTRPV1, mTRPV2, hTRPV3, hTRPV4, hTRPC6, or hTRPM8 channels. TRPA1 agonist-3 alleviates inflammatory pain in mice through a channel desensitization mechanism.

Methyl kakuol shows agonistic activity against TRPA1 with an EC₅₀ of 0.27 µM.

Neoambrosin is a sesquiterpene lactone. Neoambrosin acts as a partial agonist of PPARγ and TRPA1 receptors, with no carbonic anhydrase inhibitory activity. Neoambrosin can be used in research on hypoglycemia, analgesia, anti-inflammation and anticancer effects.

Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC₅₀=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce apoptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.