TRP Channel Agonist

TRPV4 agonist-1 is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 of 60 nM in the hTRPV4 Ca2+ assay[1].

TRPM8 agonist WS-3 (Standard) is the analytical standard of TRPM8 agonist WS-3. This product is intended for research and analytical applications. TRPM8 agonist WS-3 is an specific agonist of TRPM8 with an EC₅₀ of 3.7 μM. TRPM8 agonist WS-3 inhibits epileptic seizures through a TRPM8 dependent mechanism. TRPM8 agonist WS-3 can be used for research on epilepsy and other conditions.

D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.

Capsaicin-d₃ is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin induces a nociceptive response by binding to its receptors. Capsaicin has analgesic effects on neurological disorders. Capsaicin has antioxidant, anti-inflammatory, anti-cancer effects.

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

Polygodial pyridazine (compound 7) is a polygodial analogue and a TRPV1 agonist with a GI₅₀ of 72 μM against MCF-7. Polygodial pyridazine can be utilized in cancer research.

TRPM8 receptor agonist-1 (Example 81) is a TRPM8 receptor agonist. TRPM8 receptor agonist-1 can trigger the inward flow of calcium, sodium and other ions within the cell, causing the cell membrane to depolarize and triggering an action potential. TRPM8 receptor agonist-1 can activate signals related to the swallowing reflex and can be used for the research of oropharyngeal dysphagia.

TRPA1 agonist-2 (Compound 4B) is an orally active and highly selective TRPA1 channel agonist. TRPA1 agonist-2 triggers calcium influx and stimulates GLP-1 secretion. TRPA1 agonist-2 is promising for research of diabetes, obesity, and related neurodegenerative diseases.

Capsiconiate (Coniferyl (E)-8-methyl-6-nonenoate) is a TRPV1 agonist (EC₅₀= 3.2 μM). Capsiconiate can be used to study TRPV1-mediated diseases such as pain, inflammation, and epilepsy(EC₅₀= 3.2 μM).

AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory activity against TRPM8 noted.

Protoporphyrin IX (Standard) is the analytical standard of Protoporphyrin IX. This product is intended for research and analytical applications. Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma.

TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel.

Capsaicin (Purity 65%) (Standard) is the analytical standard of Capsaicin (Purity 65%). This product is intended for research and analytical applications. Capsaicin (Purity 65%) is a mixture of Capsaicin and Dihydrocapsaicin (Ratio >2:1).Capsaicin (Purity 65%) is an orally active capsaicin receptor (TRPV1) agonist.

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.

JYL 1511 is a partial agonist of vanilloid receptor VR1.

Capsaicin-d₇ is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin induces a nociceptive response by binding to its receptors. Capsaicin has analgesic effects on neurological disorders. Capsaicin has antioxidant, anti-inflammatory, anti-cancer effects.

OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a K_i of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC₅₀ of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (K_i=4.9 μM).

Farnesyl pyrophosphate is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.

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.

Dehydroisoandrosterone 3-acetate (Standard) is the analytical standard of Dehydroisoandrosterone 3-acetate. This product is intended for research and analytical applications. Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.