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Results for "

TRPA1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

44

Inhibitors & Agonists

12

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100965
    Diphenyleneiodonium chloride
    Maximum Cited Publications
    59 Publications Verification

    DPI

    		 TRP Channel NADPH Oxidase Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology
    Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.
    Diphenyleneiodonium chloride
  • HY-15064
    HC-030031
    35+ Cited Publications

    		 TRP Channel Neurological Disease
    HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
    HC-030031
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    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 .
    Lazertinib
  • HY-121636
    Resolvin D2
    5 Publications Verification

    RvD2

    		 TRP Channel Infection Neurological Disease Inflammation/Immunology
    Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons .
    Resolvin D2
  • HY-101507
    Zerencotrep
    10+ Cited Publications

    Pico145; HC-608

    		 TRP Channel Cancer
    Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 .
    Zerencotrep
  • HY-165559
    Trpvicin

    		TRP Channel Inflammation/Immunology
    Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC50s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology .
    Trpvicin
  • HY-N10319
    Artepillin C

    		Epigenetic Reader Domain Necroptosis TRP Channel Metabolic Disease Inflammation/Immunology Cancer
    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 .
    Artepillin C
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    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 .
    Lazertinib mesylate
  • HY-171846
    LY3526318

    		TRP Channel Neurological Disease Inflammation/Immunology
    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 .
    LY3526318
  • HY-W002116
    Methyl syringate

    		TRP Channel COX Phosphatase Bacterial Infection Metabolic Disease Inflammation/Immunology Cancer
    Methyl syringate is a selective TRPA1 agonist. Methyl syringate regulates food intake and gastric emptying through a TRPA1-mediated pathway. Methyl syringate is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a chemical marker of Asphodel monofloral honey. Methyl syringate contributes to the antibacterial activity of honey. Methyl syringate inhibits aflatoxin production. Methyl syringate can contribute to weight suppression. Methyl syringate can be studies for cancer prevention (e.g. lung cancer), suppression of hypoxia-induced inflammatory response and tumorigenesis .
    Methyl syringate
  • HY-B1177
    Crotamiton

    		Environmental Pollutants TRP Channel Parasite Infection
    Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .
    Crotamiton
  • HY-156684
    Nedizantrep

    GDC-6599

    		 TRP Channel Neurological Disease
    GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guinea pigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough .
    Nedizantrep
  • HY-W014421
    AP-18
    2 Publications Verification

    		 TRP Channel Neurological Disease
    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 .
    AP-18
  • HY-B1173
    (+)-Camphor
    1 Publications Verification

    D-(+)-Camphor; (1R)-(+)-Camphor

    		 Environmental Pollutants Bacterial Neurological Disease Inflammation/Immunology Cancer
    (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
    (+)-Camphor
  • HY-148236
    BAY-390
    1 Publications Verification

    		 TRP Channel Inflammation/Immunology
    BAY-390, a chemical probe, is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation .
    BAY-390
  • HY-126941
    Hecogenin acetate

    		ERK MMP Reactive Oxygen Species (ROS) NF-κB p38 MAPK NOD-like Receptor (NLR) TRP Channel TNF Receptor Interleukin Related Infection Neurological Disease Inflammation/Immunology Endocrinology
    Hecogenin acetate is an orally active steroid saponin aglycone with extensive biological activities. Hecogenin acetate inhibits the phosphorylation of NF-κB and p38 MAPK signaling pathways, antagonizes TRPA1/TRPM8 channels, inhibits the production of pro-inflammatory cytokines, and has anti-inflammatory and analgesic effects. Hecogenin acetate inhibits the production of ROS and the activation of NLRP3 inflammasome; downregulates the expression of MMP-2, and has neuroprotective and anti-tumor activities. Hecogenin acetate enhances gastric mucosal defense and promotes ulcer healing. Hecogenin acetate can be used in combination with certain antibiotics to regulate bacterial efflux pumps and restore antibiotic sensitivity .
    Hecogenin acetate
  • HY-N10319R
    Artepillin C (Standard)

    		Reference Standards TRP Channel Necroptosis Epigenetic Reader Domain Metabolic Disease Inflammation/Immunology Cancer
    Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. 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 apoptosis, 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 .
    Artepillin C (Standard)
  • HY-121636S
    Resolvin D2-d5

    RvD2-d5

    		 TRP Channel Infection Neurological Disease Inflammation/Immunology
    Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons .
    Resolvin D2-d5
  • HY-N10612
    Petasin

    		AMPK PPAR TRP Channel Mitochondrial Metabolism Metabolic Disease Cancer
    Petasin inhibits adipogenesis in cell 3T3-F442A with an IC50 of 0.95 μM. Petasin inhibits the expression of lipid synthesis factors ACC1, FAS and SCD1 by inhibiting transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels . Petasin inhibits mitochondrial complex I, thereby inhibiting tumor growth and metastasis. Petasin activates AMPK signaling pathway, participating in regulation of glucose and lipid metabolism. Petasin is orally active .
    Petasin
  • HY-N7536
    Voacangine

    		TRP Channel Others
    Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
    Voacangine
  • HY-115877
    GDC-0334

    		TRP Channel Others
    GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma .
    GDC-0334
  • HY-145491
    Resolvin D5

    		ERK NF-κB CCR Inflammation/Immunology
    Resolvin D5 is an anti-inflammatory and analgesic agent produced in M2 macrophages. Resolvin D5 alleviates Paclitaxel (HY-B0015)-induced mechanical allodynia and inflammatory pain by activating the GPR32 receptor, with gender specificity (effective only in male mice) and independence from TRPV1 or TRPA1 channels. Resolvin D5 attenuates LPS-induced ERK phosphorylation and NF-κB nuclear translocation, downregulates proinflammatory mediators such as IL-6 and CCL5, inhibits Th17 cell differentiation and osteoclastogenesis, promotes regulatory T cell differentiation, and shows no cytotoxicity to human monocytes. The level of Resolvin D5 is elevated in arthritic SKG mice, but Resolvin D5 has no effect on dendritic cell differentiation or M1 macrophage polarization, nor does it prevent ZyA-induced arthritis progression. Resolvin D5 is suitable for research related to chemotherapy-induced peripheral neuropathy, inflammatory pain and rheumatoid arthritis .
    Resolvin D5
  • HY-W002116S
    Methyl syringate-d6

    		TRP Channel COX Phosphatase Bacterial Infection Metabolic Disease Inflammation/Immunology Cancer
    Methyl syringate-d6 is the deuterium labeled Methyl syringate. Methyl syringate is a selective TRPA1 agonist. Methyl syringate regulates food intake and gastric emptying through a TRPA1-mediated pathway. Methyl syringate is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a chemical marker of Asphodel monofloral honey. Methyl syringate contributes to the antibacterial activity of honey. Methyl syringate inhibits aflatoxin production. Methyl syringate can contribute to weight suppression. Methyl syringate can be studies for cancer prevention (e.g. lung cancer), suppression of hypoxia-induced inflammatory response and tumorigenesis .
    Methyl syringate-d6
  • HY-W010270A
    Aurothiomalate disodium

    		TRP Channel NF-κB NO Synthase TREM receptor Arginase Metabolic Disease Inflammation/Immunology
    Aurothiomalate (disodium) is a TRPA1 inhibitor. Aurothiomalate (disodium) inhibits NF-κB activation and iNOS expression. Aurothiomalate (disodium) promotes M2 transformation of macrophages and increases the expression of TREM-2 and arginase-1. Aurothiomalate (disodium) can be used in the study of liver fibrosis/cirrhosis and arthritis .
    Aurothiomalate disodium
  • HY-B1173R
    (+)-Camphor (Standard)

    D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)

    		 Reference Standards Bacterial Neurological Disease Inflammation/Immunology Cancer
    (+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
    (+)-Camphor (Standard)
  • HY-W008356
    2-Fluoro-4-iodobenzonitrile

    		Drug Intermediate Infection Metabolic Disease
    2-Fluoro-4-iodobenzonitrile is a building block, which can be used to synthesize L. infantum trypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors. 2-Fluoro-4-iodo benzonitrile can also be used to synthesize transient receptor potential ankyrin 1 (TRPA1) antagonists .
    2-Fluoro-4-iodobenzonitrile
  • HY-172898
    TRPA1-IN-4

    		TRP Channel Neurological Disease
    TRPA1-IN-4 (12) is a TRPA1 inhibitor, with an IC50 of 45 nM. TRPA1-IN-4 (12) can be used in the pain research .
    TRPA1-IN-4
  • HY-159134
    TRPA1-IN-3

    		TRP Channel Others
    TRPA1-IN-3 (commound 1) is a TRPA1 inhibitor. TRPA1-IN-3 can be used in skin and respiratory tract related research .
    TRPA1-IN-3
  • HY-153711
    TRPA1-IN-2

    		TRP Channel Inflammation/Immunology
    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 .
    TRPA1-IN-2
  • HY-W002116R
    Methyl syringate (Standard)

    		Reference Standards TRP Channel COX Phosphatase Bacterial Infection Metabolic Disease Inflammation/Immunology Cancer
    Methyl syringate is a selective TRPA1 agonist. Methyl syringate regulates food intake and gastric emptying through a TRPA1-mediated pathway. Methyl syringate is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a chemical marker of Asphodel monofloral honey. Methyl syringate contributes to the antibacterial activity of honey. Methyl syringate inhibits aflatoxin production. Methyl syringate can contribute to weight suppression. Methyl syringate can be studies for cancer prevention (e.g. lung cancer), suppression of hypoxia-induced inflammatory response and tumorigenesis .
    Methyl syringate (Standard)
  • HY-N12605
    hTRPA1-IN-1

    		TRP Channel Neurological Disease
    hTRPA1-IN-1 (19), a norsesterterpenoid that can be isolated from the Marine Sponge Diacarnus spinipoculum, is an inhibitor of transient receptor potential Ankyrin 1 (TRPA1), with an IC50 of 2 μM .
    hTRPA1-IN-1
  • HY-15064R
    HC-030031 (Standard)

    		TRP Channel Neurological Disease
    HC-030031 (Standard) is the analytical standard of HC-030031. This product is intended for research and analytical applications. HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
    HC-030031 (Standard)
  • HY-B1177R
    Crotamiton (Standard)

    		Reference Standards Parasite TRP Channel Infection
    Crotamiton (Standard) is the analytical standard of Crotamiton. This product is intended for research and analytical applications. Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .
    Crotamiton (Standard)
  • HY-W708469
    Resolvin D2 methyl ester

    		Endogenous Metabolite TRP Channel Inflammation/Immunology
    Resolvin D2 methyl ester is an ester derivative of the DHA (HY-B2167) metabolite Resolvin D2 (HY-121636) with anti-inflammatory and anti-infective activities. Resolvin D2 is a leukocyte modulator and a potent inhibitor of neuronal TRPV1 (IC50=0.1 nM) and TRPA1 (IC50=2 nM). Resolvin D2 can be used in sepsis research .
    Resolvin D2 methyl ester
  • HY-N9503
    Carvacryl acetate

    		TRP Channel Na+/K+ ATPase Parasite Others Neurological Disease Inflammation/Immunology
    Carvacryl acetate is an orally active and brain-penetrant TRPA1 receptor activator and Na +/K +-ATPase activator. Carvacryl acetate modulates GABAergic signaling, alters hippocampal GABA and glutamine levels, reduces lipid peroxidation and nitrite formation, scavenges hydroxyl radicals, and boosts glutathione and antioxidant enzyme activity. Carvacryl acetate inhibits Haemonchus contortus larval hatching, development, adult motility, and fecal egg counts, and induces adult worm structural damage. Carvacryl acetate can be used for the research of intestinal mucositis, gastrointestinal nematode infection, epilepsy, and neurodegenerative diseases .
    Carvacryl acetate
  • HY-122692
    TRPV4/TRPA1-IN-1

    		TRP Channel Neurological Disease Inflammation/Immunology
    TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis .
    TRPV4/TRPA1-IN-1
  • HY-132184S
    5,6-Epoxyeicosatrienoic acid-d11

    5,6-EET-d11; (±)5,6-EpETrE-d11

    		 Isotope-Labeled Compounds Adrenergic Receptor Cardiovascular Disease Neurological Disease
    5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid is one of the four major epoxyeicosatrienoic acid (EET) isomers metabolized from Arachidonic acid (HY-109590). 5,6-Epoxyeicosatrienoic acid induces peripheral vasodilation and lowers blood pressure by inhibiting T-type calcium channels (Cav3.2: IC50 = 0.54 μM). 5,6-Epoxyeicosatrienoic acid causes vasoconstriction in hypoxic pulmonary blood vessels via activating Rho kinase in a membrane depolarization-dependent manner. 5,6-Epoxyeicosatrienoic acid induces mechanical pain by activating TRPA1. 5,6-Epoxyeicosatrienoic acid can be used in studies related to hypoxic pulmonary vasoconstriction, mechanical hyperalgesia and hypertension.
    5,6-Epoxyeicosatrienoic acid-d11
  • HY-15058
    AMG2504

    		TRP Channel Neurological Disease
    AMG2504 is a TRPA1 antagonist with an IC50 value of 35 nM against human TRPA1. AMG2504 inhibits human TRPA1 activation induced by AITC and noxious cold stimulation. AMG2504 is applicable to research related to chronic pain .
    AMG2504
  • HY-179503
    PDE/TRPA1/CHIT1-IN-1

    		Phosphodiesterase (PDE) TRP Channel NOD-like Receptor (NLR) NF-κB TNF Receptor Interleukin Related Inflammation/Immunology
    PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research .
    PDE/TRPA1/CHIT1-IN-1
  • HY-100965R
    Diphenyleneiodonium chloride (Standard)

    DPI (Standard)

    		 TRP Channel Reference Standards NADPH Oxidase Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology
    Diphenyleneiodonium chloride (Standard) is the analytical standard of Diphenyleneiodonium chloride (HY-100965). This product is intended for research and analytical applications. Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.
    Diphenyleneiodonium chloride (Standard)
  • HY-109061A
    Lazertinib mesylate hydrate

    YH25448 mesylate hydrate; GNS-1480 mesylate hydrate

    		 Apoptosis Akt TRP Channel EGFR ERK Cancer
    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 .
    Lazertinib mesylate hydrate
  • HY-101507R
    Zerencotrep (Standard)

    Pico145 (Standard); HC-608 (Standard)

    		 TRP Channel Reference Standards Cancer
    Zerencotrep (Standard) is the analytical standard of Zerencotrep (HY-101507). This product is intended for research and analytical applications. Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 .
    Zerencotrep (Standard)
  • HY-179432
    Cannabitwinol

    CBDD

    		 TRP Channel NF-κB Interleukin Related Neurological Disease Inflammation/Immunology
    Cannabitwinol is a selective thermosensitive TRP modulator and NF-κB inhibitor. Cannabitwinol inhibits TNFα-induced NF-κB-driven transcription and TNFα-induced IL-8 release, and exhibits anti-inflammatory and antioxidant activities. Cannabitwinol shows selectivity for cold-activated TRP channels, activating TRPA1 (EC50 = 3.0 μM) and antagonizing TRPM8 (IC50 = 3.9 μM), but has no significant affinity for heat-activated TRP channels such as TRPV1 and TRPV2. Cannabitwinol can be used in research related to inflammatory skin diseases, cold allodynia, and hyperalgesia .
    Cannabitwinol
  • HY-181762
    Multitarget AD-IN-6

    		Phosphodiesterase (PDE) TRP Channel NF-κB NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    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 Kd 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 .
    Multitarget AD-IN-6

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