TRPA1

TRPA1 Related Products (30):

By Type:	Pan (10) Selective (7)
By Effects:	Inhibitors (9) Agonists (5) Antagonists (6) Activators (8) Modulator (1)

Cat. No.	Product Name	Effect	Purity

HY-109061

Lazertinib	Activator	99.87%
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

HY-107436

LE135	Activator	99.0%
LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC₅₀s of 2.5 μM and 20 μM, respectively.

HY-W014421

AP-18	Inhibitor	99.61%
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC₅₀ of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC₅₀ of 10.3 μM.

HY-109061B

Lazertinib mesylate	Activator	99.85%
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

HY-120689

PF-04745637	Antagonist	99.97%
PF-04745637 is a potent and selective TRPA1 antagonist with an IC₅₀ of 17 nM for human TRPA1.

HY-175980

TRPA1 agonist-3	Agonist	99.78%
TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, with EC₅₀ values of 50.05 μM and 314.04 μM for human and mouse TRPA1, respectively. TRPA1 agonist-3 does not activate hTRPV1, mTRPV2, hTRPV3, hTRPV4, hTRPC6, or hTRPM8 channels. TRPA1 agonist-3 alleviates inflammatory pain in mice through a channel desensitization mechanism.

HY-109061A

Lazertinib mesylate hydrate	Activator
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

HY-181762

Multitarget AD-IN-6	Inhibitor
Multitarget AD-IN-6 (Compound 39) is a multi-target inhibitor, with an IC₅₀ of 15.54 μM against PDE4B, 15.15 μM against PDE7A, 8.39 μM against PDE3A, and a K_d of 37.7 μM against CHIT1. Multitarget AD-IN-6 acts as a TRPA1 antagonist, reduces the level of the NLRP3 inflammasome multiprotein complex to inhibit its activation, while inhibiting PDE4B, PDE7A and CHIT1, and decreasing the phosphorylation of NF-κB. Multitarget AD-IN-6 improves the pathology of elastase-induced emphysema in mice. Multitarget AD-IN-6 is applicable for the research of chronic obstructive pulmonary disease.

HY-171846

LY3526318	Inhibitor	99.92%
LY3526318 is an orally active, selective TRPA1 antagonist (IC₅₀=5-6μM). LY3526318 blocks TRPA1 channels, inhibits pain signal transduction mediated by the channel, and exerts analgesic activity. LY3526318 is mainly used in the research of chronic pain-related fields, such as diabetic peripheral neuropathy, chronic low back pain, and pain caused by osteoarthritis.

HY-N10319

Artepillin C	Agonist	98.28%
Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC₅₀=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.

HY-15065

Chembridge-5861528	Antagonist	99.12%
Chembridge-5861528 (TCS 5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC₅₀ values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities.

HY-107535

AS1269574	Activator	99.84%
AS1269574 is a potent, orally available GPR119 agonist, with an EC₅₀ of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.

HY-N7117

1,4-Cineole	Activator
1,4-Cineole is an oxygenated monoterpene found in eucalyptus oil. 1,4-Cineole is a hTRPM8 and hTRPA1 agonist. 1,4-Cineole can increase intracellular Ca²⁺ concentration. 1,4-Cineole exhibits anti-anxiety and anti-depression effects. 1,4-Cineole can be used for the research of neurological disease, such as depression .

HY-153711

TRPA1-IN-2	Inhibitor	99.82%
TRPA1-IN-2 (compound 1) is a potent and orally active TRPA1 inhibitor with an IC₅₀ value of 0.04 µM. TRPA1-IN-2 shows anti-inflammation activity.

HY-P1073

ProTx-I	Inhibitor
ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC₅₀ values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba²⁺ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.

HY-N7117R

1,4-Cineole (Standard)	Activator
1,4-Cineole (Standard) is the analytical standard of 1,4-Cineole (HY-N7117). 1,4-Cineole is an oxygenated monoterpene found in eucalyptus oil. 1,4-Cineole is a hTRPM8 and hTRPA1 agonist. 1,4-Cineole can increase intracellular Ca²⁺ concentration. 1,4-Cineole exhibits anti-anxiety and anti-depression effects. 1,4-Cineole can be used for the research of neurological disease, such as depression .

HY-172774

TRPV1 antagonist 10	Antagonist	98.54%
TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

HY-N7965

Methyl kakuol	Agonist
Methyl kakuol shows agonistic activity against TRPA1 with an EC₅₀ of 0.27 µM.

HY-162856

TRPV1-IN-2	Inhibitor
TRPV1-IN-2 ((R)-32) is a TRPV1 inhibitor. TRPV1-IN-2 has protective effects on ED epilepsy models.

HY-127003

Neoambrosin	Agonist
Neoambrosin is a sesquiterpene lactone. Neoambrosin acts as a partial agonist of PPARγ and TRPA1 receptors, with no carbonic anhydrase inhibitory activity. Neoambrosin can be used in research on hypoglycemia, analgesia, anti-inflammation and anticancer effects.

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