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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
24 Results for "
TRPA1-IN-1
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "TRPA1-IN-1" in MCE Product Catalog:
Cat. No.: HY-142214
CAS No.: 2376824-92-7
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TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
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3 Cited Publications
Synonyms: YH25448; GNS-1480
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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 .
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3 Cited Publications
Cat. No.: HY-109061B
CAS No.: 2247995-37-3
Synonyms: YH25448 mesylate; GNS-1480 mesylate
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 .
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1 Cited Publications
Cat. No.: HY-18779
CAS No.: 1332708-14-1
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PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse .
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Other Monoterpenes Terpenoids Other Diseases Plants Lauraceae Disease Research Fields Cinnamomum camphora
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(E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist .
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1 Cited Publications
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AMG2850 is an orally active, blood-brain barrier-permeable selective TRPM8 competitive antagonist. AMG2850 abolishes the counterirritant effect of TRPM8 agonists, blocks TRPM8 activation induced by cold, (-)-Menthol (HY-75161) and Icilin (HY-11062), and exhibits selectivity over TRPA1, TRPV1, TRPV3 and TRPV4. AMG2850 is applicable for pain-related research .
Cat. No.: HY-W002116
CAS No.: 884-35-5
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Monophenols Animals Vitis vinifera cv. Zalema Phenols Plants Vitaceae Disease Research Fields Inflammation/Immunology
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Cat. No.: HY-115877
CAS No.: 1984824-54-5
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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 .
Cat. No.: HY-W002116S
CAS No.: 1182838-09-0
Cat. No.: HY-111494
CAS No.: 1984825-08-2
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TRPA1 Antagonist 1 is a methylene phosphate proagent which converts to its active parent agent, a TRPA1 antagonist with an IC50 of 8 nM.
Cat. No.: HY-W008356
CAS No.: 137553-42-5
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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 .
Cat. No.: HY-P10356
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Synonyms: D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)
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Cat. No.: HY-122692
CAS No.: 1532515-60-8
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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 .
Cat. No.: HY-173471
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TRPA1 agonist-1 (compound 21) is a potent and selective TAAR1 agonist with an EC50 of 25.47 μM. TRPA1 agonist-1 shows effective analgesic properties without irritation in mice .
Cat. No.: HY-W002116R
CAS No.: 884-35-5
Cat. No.: HY-15056
CAS No.: 118215-82-0
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AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory activity against TRPM8 noted .
Cat. No.: HY-179503
Target:
Phosphodiesterase (PDE) TRP Channel NOD-like Receptor (NLR) NF-κB TNF Receptor Interleukin Related
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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 .
Cat. No.: HY-187167
CAS No.: 3136943-00-2
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TRPA1-IN-5 is a TRPA1 inhibitor with inhibitory activity against TRPA1. TRPA1-IN-5 has pharmacokinetic and pharmacodynamic activities .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
