trpa 1

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.

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

TRPA1-IN-4 (12) is an inhibitor of TRPA1, with an IC50 of 45 nM, utilized in pain research.

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.

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.

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.

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.

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

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.

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.

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).

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).