trpa1 in 1

TRPA1-IN-1 is a potent and selective antagonist of the TRPA1 channel, with significant oral bioavailability as a small molecule.

TRPA1 agonist-1 (compound 21) is an effective and selective TAAR1 agonist with an EC50 of 25.47 μM, exhibiting significant non-irritant analgesic properties in mice.

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.

PDE/TRPA1/CHIT1-IN-1 is an inhibitor of PDEs, TRPA1, and hCHIT1 with a KD value of 37.7 μM. It acts as a broad-spectrum PDE inhibitor, effectively targeting key subtypes including PDE4B, PDE7A, PDE3A, and PDE8A with IC50 values of 15.54, 15.15, 8.39, and 16.46 μM, respectively. By inhibiting NLRP3 inflammasome activation and blocking NF-κB phosphorylation, PDE/TRPA1/CHIT1-IN-1 downregulates the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. This compound is useful for research into chronic obstructive pulmonary disease (COPD) and related inflammatory lung conditions.

TRPA1 Antagonist 1 is an antagonist of TRPA1(IC50: 8 nM) and is a methylene phosphate prodrug which converts to its active parent drug.

TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, exhibiting EC50 values of 50.05 μM for human TRPA1 and 314.04 μM for mouse TRPA1 in HEK-293T cells. This compound does not activate hTRPV1, mTRPV2, hTRPV3, hTRPV4, hTRPC6, or hTRPM8 channels. Additionally, TRPA1 agonist-3 alleviates inflammatory pain in mice through channel desensitization mechanisms.

TRPA1 Antagonist 3 is a compound with photoswitchable properties that acts as an agonist on the TRPA1 channel, providing the ability for optical control.

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.

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

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.

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC50 value of 8.1. It displays excellent selectivity for related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4) with selectivity greater than 100-fold. TRPM5 agonist-1 induces local stimulation of gastrointestinal transit in mice and is useful for studying the promotion of gastric motility.

GRC-17536 is an orally available, potent, and selective transient receptor potential anchor protein 1 (TRPA1) inhibitor that has been shown to be highly effective in the treatment of inflammation and neuropathic pain in animal models. The selectivity of G

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)

IAA65 is a potent and highly selective transient receptor potential ankyrin 1 (TRPA1) inhibitor (IC50 = 4.3 nM). It demonstrates significant analgesic activity in animal models of inflammatory and neuropathic pain by competitively blocking TRPA1-mediated calcium influx in sensory neurons.

Supercinnamaldehyde is a transient receptor potential anchor protein 1 (TRPA1) activator with thousands of anticancer and antimicrobial activities.Supercinnamaldehyde inhibits NF-κB signaling, induces cytoprotective responses and suppresses inflammatory responses through Nrf2 induction.Supercinnamaldehyde has been used in the study of bacterial infections.

Dimethylamiloride hydrochloride selectively inhibits Na⁺/H⁺ exchangers located in cellular membranes, leading to intracellular H⁺ retention and a reduction in intracellular pH, Dimethylamiloride hydrochloride additionally blocks TRPA1 ion channels with an IC50 of 80 µM, making it a valuable pharmacological tool for studying ion transport, pH homeostasis, sensory signaling, and inflammatory pain mechanisms.

Wasabi Receptor Toxin (WaTx) activates TRPA1 through prolonged channel openings while reducing Ca2+ permeability. This compound has potential applications in studying both acute and persistent pain [1].

TRPA1-IN-3 (compound 1) is an inhibitor of TRPA1. It is utilized in research related to skin and respiratory pathways.

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.

(±)-Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1), it selectively reduces inflammation-induced hypermotility in vivo in a manner that is not dependent on cannabinoid receptors or TRPA1.