trpa1

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

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.

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.

Methyl syringate (Syringic Acid Methyl Ester) has a unique inhibitory activity toward aflatoxin production with a different mode of action from that of gallic acid. Methyl syringate from K. pictus is a specific and selective activator of hTRPA1, can regulate food intake and gastric emptying through a TRPA1-mediated pathway and, by extension, can contribute to weight suppression.

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.

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

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.

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).

(E)-Cardamonin (Alpinetin chalcone) is a chalconoid that has been isolated from several plants including Alpinia katsumadai and Alpinia conchigera. It is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM. It has received growing attention from the scientific community due to the expectations toward its benefits to human health.

Diphenyleneiodonium chloride (DPI)(DPI) is an irreversible inhibitor of iNOS and eNOS (IC50 values of 50 nM and 0.3 μM, respectively),and displays broad-spectrum bactericidal activity.

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.

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

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.

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

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

Hydroxy-α-sanshool is an alkyl amide isolated from the pepper. It acts as a TRPA1 covalent and TRPV1 non-covalent agonist (EC50s: 69 and 1.1 μM).

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.

Methyl Kakuol is an agonist of TRPA1 with an EC50 of 0.27 µM and can be used in studies about acting as an active ingredient in MBST constituent Asiasari Radix.

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

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)

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.

GDC-6599 (Example 8) is an orally active TRPA1 channel inhibitor, potentially useful for researching TRPA1-mediated conditions, including pain [1].

4-(Phenyldiazenyl)benzoic acid is a photosensitive and photoswitchable TRPA1 agonist used as a pharmacological tool to study pain signaling.

Optovin is a TRPA1 activator, which is reversibly photoactivated.

(±)-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.

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.

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

BAY-390 is a brain-penetrating, species-agnostic inhibitor of TRPA1, exhibiting selective inhibition of human and rat TRPA1 with IC50 values of 16 nM for hTRPA1 FLIPR, 82 nM for hTRPA1 Ephys, 63 nM for rTRPA1 FLIPR, and 35 nM for rDRG Ephys. It holds potential for inflammation research applications.

RQ-00203078 is a highly selective, potent, and orally available TRPM8 antagonist.

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].

GDC-0334 is a TRPA1 antagonist useful in treatment TRPA1-mediated diseases, such as pain or asthma.

AMG9090 is a transient receptor potential ankyrin 1 (TRPA1) antagonist.

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.

AMG2504 is a TRPA1 inhibitor.

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.

ASP7663 is a TRPA1 Receptor Agonist and exhibiting an abdominal analgesic effect in vivo.

LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), showing higher affinity for RARβ. It is highly selective over RARγ, RXRα, RXRβ, and RXRγ. LE135 also acts as a potent TRPV1 and TRPA1 receptor activator with EC50s of 2.5 μM and 20 μM, respectively.

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.