trpa1-in-2

TRPA1-IN-2 is a potent and orally active TRPA1 inhibitor with an IC50 value of 0.04 µM.TRPA1-IN-2 has anti-inflammatory activity.

1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

Trpvicin is a potent and subtype-selective TRPV3 inhibitor, exhibiting IC50 values of 0.41 μM for hTRPV3-WT and 0.22 μM for hTRPV3-G573S mutants. It shows only weak inhibitory effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1, and TRPM8). By binding to the VSLD-PD site, Trpvicin stabilizes the closed state of TRPV3 channels, and in the G573S mutant, it enters the central cavity, enhancing inhibition through symmetry restructuring and pore blockage. In mouse models, Trpvicin can inhibit itching and hair loss and is applicable for research related to inflammation and immunology.

TRPA1 agonist-2 (Compound 4B) is an orally bioavailable and highly selective activator of the TRPA1 channel. It induces calcium ion influx and stimulates GLP-1 secretion. This compound shows potential for research in diabetes, obesity, and related neurodegenerative diseases.

2-Fluoro-4-iodo benzonitrile is a building block.1,2It has been used in the synthesis ofL. infantumtrypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors.12-Fluoro-4-iodo benzonitrile has also been used in the synthesis of transient receptor potential ankyrin 1 (TRPA1) antagonists.2 1.Revuelto, A., Ruiz-Santaquiteria, M., de Lucio, H., et al.Pyrrolopyrimidine vs imidazole-phenyl-thiazole scaffolds in nonpeptidic dimerization inhibitors of Leishmania infantum trypanothione reductaseACS Infect. Dis.5(6)873-891(2019) 2.Vallin, K.S., Sterky, K.J., Nyman, E., et al.N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptorBioorg. Med. Chem. Lett.22(17)5485-5492(2012)

Pulegone (Standard) is a reference standard for research and analysis in studies involving Pulegone. 1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

hTRPA1-IN-1 (19) is a sesquiterpene compound isolated from the sponge Diacarnus spinipoculum, functioning as an inhibitor of the transient receptor potential cation channel subfamily A member 1 (TRPA1), with an IC50 of 2 μM.