Catalog No.
Product Name
Application
Product Information
Citations
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TRPM8 antagonist
TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes. - Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
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TRPA1 activatior/TRPM8 blocker
Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility. - (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
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Stable Isotope
Capsaicin-d3 is a deuterated form of Capsaicin, a well-known TRPV1 agonist derived from chili peppers. This stable isotope allows for precise tracking and analysis in various research applications. Capsaicin-d3 has been implicated in studies exploring analgesic effects for neurological disorders, as well as its potential antioxidant, anti-inflammatory, and anti-cancer properties. Its use in research facilitates a better understanding of pain pathways and the therapeutic potential of capsaicin-related compounds. -
TRPML Modulator
TRPML modulator 1 is a selective modulator of the TRPML channel, known for its role in promoting autophagy. With an AC50 of less than 2 mM in the TFEB assay, it effectively enhances autophagic flux, making it a valuable tool for research applications focused on cellular degradation processes and lysosomal function. This compound is instrumental in studying the molecular mechanisms underlying autophagy-related diseases. -
PPARγ/TRPA1 Receptor Partial Agonist
Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics. -
PPAR Agonist
20-HEPE is a metabolite of eicosapentaenoic acid that functions primarily as a peroxisome proliferator-activated receptor α (PPARα) agonist. At a concentration of 10 μM, it effectively activates PPARα in COS-7 cells that express a luciferase reporter gene. Additionally, 20-HEPE activates the mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro, although it does not exhibit analgesic effects in rat models. This compound has potential applications in the study of metabolic processes and receptor signaling pathways. -
Inflammation Inhibitor
Resolvin D5 is an anti-inflammatory agent primarily targeting the GPR32 receptor, effectively modulating inflammation responses. It alleviates Paclitaxel-induced mechanical allodynia and inflammatory pain in male mice through mechanisms that do not involve TRPV1 or TRPA1 channels. Resolvin D5 reduces LPS-induced ERK phosphorylation and NF-κB nuclear translocation while downregulating pro-inflammatory mediators, inhibiting Th17 differentiation, and promoting regulatory T cell differentiation. This compound is particularly relevant for research on chemotherapy-induced peripheral neuropathy, inflammatory pain, and rheumatoid arthritis. -
NF-κB Inhibitor/TRP Modulator
Cannabitwinol is a selective NF-κB inhibitor and thermosensitive TRP modulator. It effectively inhibits TNFα-induced NF-κB-driven transcription and IL-8 release, exhibiting notable anti-inflammatory and antioxidant properties. Cannabitwinol selectively activates cold-activated TRP channels, such as TRPA1 (EC50 = 3.0 μM), while antagonizing TRPM8 (IC50 = 3.9 μM), with minimal interaction with heat-activated TRP channels like TRPV1 and TRPV2. This compound is applicable in research focused on inflammatory skin diseases, cold allodynia, and hyperalgesia. -
TRPA1 Agonist
Methyl syringate is a selective agonist of the TRPA1 receptor, playing a crucial role in the regulation of food intake and gastric emptying through TRPA1-mediated pathways. Additionally, this compound functions as an effective phenolic mediator for bacterial and fungal laccases, enhancing their catalytic activities. Methyl syringate serves as a chemical marker in Asphodel monofloral honey and is associated with its antibacterial properties. Furthermore, it has been shown to inhibit aflatoxin production and may contribute to weight suppression, as well as being applicable in research focused on cancer prevention, hypoxia-induced inflammatory response, and tumorigenesis. -
NMDAR/TRPM4 Inhibitor
Brophenexin free base is a potent inhibitor targeting the N-methyl-D-aspartate receptor (NMDAR) and the transient receptor potential melastatin 4 (TRPM4). This compound exhibits significant neuroprotective activity, preventing NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Furthermore, Brophenexin free base has demonstrated protective effects in vivo, safeguarding against brain damage induced by middle cerebral artery occlusion (MCAO) and preserving retinal ganglion cells from NMDA-induced loss. -
Histamine H1 Receptor/TRPV1 Inhibitor
Dexbrompheniramine is a dual inhibitor of the histamine H1 receptor and the TRPV1 receptor, enabling it to effectively cross the blood-brain barrier. It functions by blocking H1 receptor activity and inhibiting TRPV1-mediated calcium responses in a dose-dependent manner, including responses triggered by Capsaicin. Research indicates that Dexbrompheniramine, when combined with Cimetidine, can mitigate drinking behavior induced by histamine and sham feeding, while it alone does not induce thirst. This compound is valuable for investigating the pathophysiology of chronic cough and related disorders. -
TRPV1 Antagonist
DWP-05195 is a TRPV1 antagonist that inhibits pain signal transduction, providing research applications in pain management studies. Additionally, DWP-05195 induces endoplasmic reticulum (ER) stress-dependent apoptosis in human ovarian cancer cells, mediated by the ROS-p38-CHOP signaling pathway. This compound may be useful for investigating both nociceptive mechanisms and potential therapeutic strategies for ovarian cancer. -
NAAA Inhibitor
AM9053 is a selective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) with an IC50 of 30 nM. It shows limited impact on FAAH activity (IC50 > 100 nM). AM9053 demonstrates significant anti-proliferative effects on colorectal cancer cells through the activation of PPAR-α and TRPV1-dependent pathways, leading to S-phase cell cycle arrest. Additionally, it alleviates intestinal fibrosis by modulating macrophage activity and inhibiting the IL-23 signaling pathway, resulting in increased levels of N-acylethanolamines, particularly palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). AM9053 is valuable for research into colorectal cancer and intestinal fibrosis. -
Endogenous Metabolite
Stearoyl serotonin is a hybrid compound designed to target the endogenous metabolite systems and is structurally derived from arachidonoyl serotonin. This compound is investigated for its ability to function as a dual antagonist of fatty acid amide hydrolase (FAAH) and the TRPV1 channel, which are critical pathways in the modulation of pain. Preliminary studies suggest that modifications to the arachidonoyl structure, such as the introduction of an 18-carbon stearoyl moiety, may influence TRPV1 channel activity; replacement with saturated fatty acids has demonstrated significant inhibition of capsaicin-induced activation. This positions stearoyl serotonin as a potential candidate for research into pain mechanisms and therapeutic applications. -
Endogenous Metabolite
SU200 is a TRPV1 agonist that modulates intracellular calcium ion concentrations. It induces distinct calcium ion response patterns, displaying notable reactivity and peak efficacy. The effects of SU200 exhibit varying degrees of response delay and variability across different cell types. This compound offers potential avenues for pharmacological development and further research into calcium signaling pathways. -
TRPM2 Agonist
Farnesyl pyrophosphate ammonium is an agonist of the TRPM2 channel, facilitating calcium influx and promoting cell death. It serves as a crucial intermediate in the mevalonate pathway, with significant roles in cholesterol and ubiquinone synthesis, as well as protein farnesylation. This compound is utilized in research focusing on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders. -
TRPC6 Activator
Hyperforin dicyclohexylammonium salt is a selective activator of transient receptor potential canonical 6 (TRPC6) channels. By modulating Ca2+ flux, this compound influences a variety of biological processes and exhibits notable pharmacological activities, including anti-depression, anti-tumor, anti-dementia, and anti-diabetic effects. Additionally, Hyperforin dicyclohexylammonium salt has been shown to enhance the secretion of IL-17α from γδ T cells and demonstrates efficacy in improving psoriasis-like symptoms in the Imiquimod-induced mouse model. This compound serves as a valuable tool in research focused on calcium signaling and related therapeutic applications. -
TRPV1 Antagonist
A-425619 is a selective antagonist of the transient receptor potential type V1 (TRPV1), exhibiting oral bioactivity. It effectively inhibits capsaicin- and N-arachidonoyl-dopamine (NADA)-induced calcium influx in both dorsal root ganglia and trigeminal ganglia. A-425619 demonstrates efficacy in alleviating pathophysiological pain linked to inflammation and tissue injury in preclinical models. This compound is valuable for researching pain mechanisms associated with inflammatory conditions. -
TRPM2 Agonist
Farnesyl pyrophosphate is an agonist of the TRPM2 channel, initiating calcium influx and promoting cell death. As a vital intermediate in the mevalonate pathway, it plays a crucial role in cholesterol and ubiquinone synthesis, as well as protein farnesylation and geranylgeranyl pyrophosphate synthesis. Farnesyl pyrophosphate is utilized in research focused on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, and the study of inflammation and autoimmune disorders. -
TRPV3 Inhibitor
Trpvicin is a selective inhibitor of the TRPV3 channel, demonstrating IC50 values of 0.41 μM and 0.22 μM for human TRPV3-WT and the hTRPV3-G573S mutant, respectively. Its mechanism of action involves stabilizing TRPV3 in a closed conformation primarily through VSLD-PD binding, while also engaging alternative binding sites in the G573S mutant to impede channel activity. Trpvicin exhibits minimal off-target effects on other TRP family members, making it a valuable tool for studying inflammation, immunology, and conditions associated with itch and hair loss in mouse models. -
TRPA1 Channel Antagonist
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain. -
TRPM3 Inhibitor
TRPM3-IN-1 is a potent inhibitor of the TRPM3 ion channel, exhibiting an IC50 value of less than 1 µM. This compound is valuable for research focused on the modulation of pain mechanisms and inflammatory responses. Its ability to selectively target TRPM3 makes it a promising tool for investigating related biological pathways and potential therapeutic applications. -
TRPML1 Agonist
ML-SA5 is a potent agonist of the TRPML1 cation channel, effectively activating the endosomal TRPML1 current in DMD myocytes with an EC50 of 285 nM. This compound demonstrates significant anticancer activity by inhibiting tumor growth, making it valuable for research applications aimed at exploring TRPML1 functions and their implications in cancer biology and muscle disorders. -
TRPC Agonist
IA-Alkyne is a TRPC channel (TRPC) agonist that facilitates the investigation of respiratory infections through enhanced channel activity. This compound serves as a versatile chemical probe for quantitative profiling of cysteine reactivity, enabling isotopic tagging. Additionally, IA-Alkyne features an alkyne functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in various biological research studies. -
TRPM3 Agonist
CIM0216 is a selective agonist of the TRPM3 ion channel, demonstrating potent stimulation specifically for this target over other TRPM family members such as TRPM1, TRPM2, and TRPM4-8. It activates TRPM3-dependent pathways to induce pain and facilitate the release of neuropeptides from sensory nerve terminals in vitro. This compound serves as an important research tool for investigating the physiological roles of TRPM3 and has applications in the study of neurogenic inflammation. -
TRPC6 Antagonist
BI-749327 is a potent and highly selective antagonist of the TRPC6 channel, exhibiting IC50 values of 13 nM for mouse TRPC6, 19 nM for human TRPC6, and 15 nM for guinea pig TRPC6. This compound demonstrates an 85-fold selectivity for mouse TRPC6 over TRPC3 and a 42-fold selectivity over TRPC7. Due to its oral bioavailability and inhibition of TRPC6, BI-749327 is suitable for research applications involving ion channel modulation and the investigation of associated physiological and pathological processes. -
TRPML1/2/3 Inhibitor
(1R,2R)-ML-SI3 is a selective inhibitor of the TRPML1, TRPML2, and TRPML3 ion channels, with IC50 values of 1.6 μM, 2.3 μM, and 12.5 μM, respectively. This compound is valuable for investigating the physiological roles of TRPML channels in cellular signaling and ion homeostasis. It is well-suited for research applications related to lysosomal function, calcium signaling, and potential therapeutic strategies targeting lysosomal storage disorders. -
TRPV2 Antagonist
SET2 is a selective antagonist of the TRPV2 channel, with an IC50 value of 0.46 μM. This compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. Additionally, SET2 diminishes lysophosphatidic acid (LPA)-induced increases in cytoplasmic calcium levels, making it useful for research focused on cancer biology and calcium signaling pathways. -
TRPV4 Antagonist
GSK205 is a selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4) channel, exhibiting an IC50 of 4.19 μM for TRPV4-mediated calcium influx inhibition. This compound is instrumental in studying TRPV4's role in various physiological and pathological processes, including pain sensation, inflammation, and cellular mechanotransduction. GSK205 is a valuable tool for researchers investigating the therapeutic potential of TRPV4 modulation in various disease models. -
TRPM2 Inihibitor
JNJ-28583113 is a potent TRPM2 inhibitor that exhibits permeability across the blood-brain barrier. By inhibiting TRPM2, JNJ-28583113 effectively blocks the phosphorylation of GSK3α and β subunits, offering protective effects against oxidative stress-induced cell death. Additionally, it reduces cytokine release from microglia in response to pro-inflammatory stimuli, making it a valuable tool for research in neuroinflammation and oxidative stress pathways. -
TRPM8 Channel Blocker
AMTB hydrochloride is a selective antagonist of the TRPM8 channel, effectively inhibiting icilin-induced TRPM8 activation with a pIC50 of 6.23. This reagent is valuable in the study of overactive bladder conditions and painful bladder syndrome. Additionally, AMTB hydrochloride exhibits non-selective inhibition of voltage-gated sodium channels, providing a broader context for its use in electrophysiological research. -
TRPC3 Agonist
GSK1702934A is a selective agonist of the TRPC3 ion channel. It enhances cardiac contractility and plays a role in the modulation of arrhythmogenesis through TRPC3 activation. This compound is valuable for research applications investigating cardiac function and the physiological effects of TRPC3 modulation in various disease models. -
TRPA1/TRPV1 Agonist
Hydroxy-α-sanshool is an agonist of the transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) channels, exhibiting EC50 values of 69 μM and 1.1 μM, respectively. This compound plays a significant role in pain research by activating these nociceptive pathways, potentially contributing to studies on pain sensation and modulation. -
TRPC4/5 Activator
Englerin A is a selective activator of TRPC4 and TRPC5 channels, exhibiting EC50 values of 11.2 nM and 7.6 nM, respectively. This compound is known to induce cell death in renal carcinoma cells through the mechanism of increased calcium influx and subsequent calcium overload. Englerin A serves as a valuable tool for investigating TRPC channel function and potential therapeutic approaches in cancer research. -
RARβ/RARα Antagonist
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts. -
TRPV2 Blocker
TRPV2-selective blocker 1 is a selective inhibitor of the transient receptor potential vanilloid 2 (TRPV2) channel, exhibiting an IC50 of 6.3 μM. This compound selectively targets TRPV2 without affecting TRPV1, TRPV3, or TRPV4 channels. Its primary biological activities include blocking TRPV2-mediated Ca2+ influx in macrophages and inhibiting macrophage phagocytosis, making it a valuable tool for research on immune responses and cellular signaling pathways involving TRPV2. -
TRPML1 Agonist
MK6-83 is a potent agonist of TRPML1, exhibiting enhanced efficacy and activity. This compound exhibits potential for research into Mucolipidosis type IV, facilitating investigations into the physiological role of TRPML1 and its implications in related pathologies. Its use may contribute to a deeper understanding of lysosomal function and associated disorders. -
TRPM4 Inhibitor
TRPM4-IN-2 is a potent inhibitor of the transient receptor potential melastatin 4 (TRPM4) channel, exhibiting an IC50 value of 0.16 µM. This compound is particularly relevant in the study of prostate and colorectal cancers, providing valuable insights into TRPM4's role in tumor biology and potential therapeutic pathways. Its ability to modulate TRPM4 activity makes it a useful tool in cancer research and drug development. -
TRPA1 Channel Activator
Umbellulone is a potent TRPA1 channel activator derived from the leaves of Umbellularia californica. This compound selectively stimulates TRPA1 channels in peptidergic, nociceptive neurons, thereby activating the trigeminovascular system. Umbellulone is valuable for research applications focused on pain signaling pathways and the mechanisms underlying migraine and other pain-related disorders. -
TRPV1 Activator
N-Oleoyldopamine is an oral TRPV1 activator and 5-lipoxygenase (5-LOX) inhibitor that effectively crosses the blood-brain barrier. It stimulates histaminergic neurons in the tuberomammillary nucleus via a dopamine receptor mechanism, independent of TRPV1 and cannabinoid receptors. N-Oleoyldopamine enhances insulin release and promotes glucose-dependent insulinotropic polypeptide through a GPR119-dependent pathway, thus improving glucose tolerance. Additionally, it benefits cardiovascular health by mitigating left ventricular dysfunction and reducing myocardial infarction size through the release of substance P and calcitonin gene-related peptide. This compound is valuable for research into glycemic control and myocardial ischemia-reperfusion injury. -
TRPV1/A1 Inhibitor
Resolvin D2 is a potent TRPV1 and TRPA1 inhibitor with a primary mechanism targeting these transient receptor potential channels in primary sensory neurons. As a metabolite of docosahexaenoic acid (DHA), it exhibits significant anti-inflammatory and anti-infective properties, effectively regulating leukocyte function and controlling microbial sepsis. This compound's high potency and specificity make it a valuable tool in research focused on pain modulation and inflammatory responses. -
TRPM4 Inhibitor
TRPM4-IN-1 is a selective inhibitor of the TRPM4 ion channel, exhibiting an IC50 value of 1.5 μM. This compound is primarily utilized in studies related to cardiac diseases and prostate cancer, facilitating insights into the role of TRPM4 in these conditions. Its potency makes it a valuable tool for investigating the modulation of calcium signaling pathways in various biological contexts.
