TRPV1 Activator

Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.

LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC₅₀s of 2.5 μM and 20 μM, respectively.

N-Arachidonyldopamine acts as an Anandamide (HY-10863) membrane transport inhibitor, a selective CB₁ cannabinoid receptor agonist, and a VR1 receptor activator. It exhibits an EC₅₀ value of 48 nM for rat VR1 and a K_i value of 0.25 μM for CB1. N-Arachidonyldopamine exists in mammalian neural tissues. It stimulates intracellular Ca²⁺ mobilization, mediates cannabinoid-like effects, and induces hypothermia, hypomotility, catalepsy, analgesia, and hyperalgesia to heat. N-Arachidonyldopamine possesses anticancer activity against breast cancer. It can be used in research related to breast cancer and heat hyperalgesia.

N-Arachidonoyl Taurine is an activator of the transient receptor potential vanilloid TRPV1 and TRPV4, with EC₅₀s value of 28 μM and 21 μM, respectively.
The product specifications provided below refer solely to the active content of N-Arachidonoyl Taurine.

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.

AM9053 is a selective NAAA inhibitor. AM9053 inhibits NAAA catalytic activity, reduces N-acylethanolamine degradation and elevates PEA/OEA levels, indirectly activating PPAR-α and TRPV1, thereby exerting antiproliferative effects. AM9053 reduces LPS-induced nitrite production in microglia, counteracts colitis, and attenuates TNBS-induced intestinal fibrosis disease activity, collagen deposition, and fibrosis-related gene expression. AM9053 modulates macrophage polarization, macrophage-fibroblast crosstalk, T helper cell subset balance, IL-23/STAT3 signaling, and EMT-related genes. AM9053 inhibits colorectal cancer proliferation and migration, induces S phase arrest, downregulates cyclin A2/CDK2, and reduces xenograft tumor growth and azoxymethane-induced colon tumorigenesis. AM9053 can be used for research on colitis, intestinal fibrosis, and colorectal cancer.

SRP-001 is a blood-brain barrier-permeable and orally effective FAAH inhibitor and analgesic. SRP-001 avoids the CYP450-mediated formation of the hepatotoxic metabolite NAPQI, and primarily promotes the synthesis of AM404 in the periaqueductal gray by inhibiting FAAH, thereby modulating the endocannabinoid system and the TRPV1- and CB1 receptor-mediated pain network. SRP-001 can be used for research on pain and fever.

20-Hydroxy-N-arachidonoyl taurine (Compound C20:4 NAT) acts as an activator of TRPV1 and TRPV4, with EC₅₀ values of 28 µM and 21 µM, respectively. 20-Hydroxy-N-arachidonoyl taurine serves as a substrate for fatty acid amide hydrolase (FAAH).

4,5-Di-O-caffeoylquinic acid (4,5-di-O-CQA) is a natural product with multiple activities including anti-inflammatory, antioxidant, and antibacterial properties. 4,5-Di-O-caffeoylquinic acid induces intracellular Ca²⁺ influx, and inhibits hypoxia-induced COX-2 expression and cell migration via the TRPV1-mediated pathway. 4,5-Di-O-caffeoylquinic acid scavenges DPPH free radicals, inhibits Cu²⁺-mediated LDL oxidation, and reduces the production of TBARS. 4,5-Di-O-caffeoylquinic acid promotes intracellular ATP production, inhibits Aβ42 aggregation and β-sheet conversion, and protects neuroblastoma cells. 4,5-Di-O-caffeoylquinic acid inhibits the growth of Bacillus shigae. 4,5-Di-O-caffeoylquinic acid can be used in studies related to atherosclerosis, Alzheimer's disease, and bacterial infections.