trpa1 channel

JT010 is an effective agonist of TRPA1 (EC50 = 0.65 nM).

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 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.

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+ H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.

HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

1,4-Cineole (Isocineole) is a natural, oxygenated monoterpene. 1,4-Cineole can activate both human TRPM8 and human TRPA1.

Capsazepine is an antagonist of TRPV1 receptor ( IC50 : 562 nM). Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. It is therefore considered to be a capsaicin antagonist.

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.

Podocarpic acid is a natural product and a novel TRPA1 activator.

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

Umbellulone is a natural product isolated from Umbellularia californica, and stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

AS1269574 (AS 1269574) is a potent, orally available GPR119 agonist with potential for type 2 diabetes research.

Chembridge-5861528 (TCS 5861528) is a TRPA1 channel blocker that inhibits AITC- and 4-HNE-induced calcium influx with IC50 values of 14.3 μM and 18.7 μM, respectively.

beta-Eudesmol (Beta-Selinenol) is a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). It is a sesquiterpene that has been found in a variety of plants, including Cannabis, and has diverse biological activities.

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

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

PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel, eliciting TrpA1-mediated nocifensive behavior in mouse, with EC50 values of 97 nM and 23 nM for [rTrpA1] and [hTrpA1], respectively.

PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM [1].

Optovin is a TRPA1 activator, which is reversibly photoactivated.

Ludartin is a TRPA1 channel activator that has been found to produce anticancer effects by inducing DNA damage and a reduction of mitochondrial membrane potential.

A 967079 is a potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively.

AM-0902 is a potent and specific TRPA1 antagonist (IC50s: 71 131 nM for rTRPA1 and hTRPA1).

JC-229 is a potent and selective TbRPA1 inhibitor that can inhibit RPA1 in Trypanosoma brucei. JC-229 can be used to study human African Trypanosomiasis (HAT).

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.