trpa1 channel

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.

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.

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.

LY3526318 is an orally active, selective TRPA1 antagonist with an IC50 of 5-6 μM. It blocks the TRPA1 channel, inhibiting pain signal transduction mediated by this channel and demonstrating analgesic activity. LY3526318 is primarily utilized in research related to chronic pain, such as diabetic peripheral neuropathic pain, chronic lower back pain, and osteoarthritis-induced pain.

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.

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.

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.

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.

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).