Catalog No.
Product Name
Application
Product Information
Citations
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TRPV1 Antagonist
Libvatrep is a selective TRPV1 antagonist that inhibits the activity of the transient receptor potential vanilloid 1 channel. It exhibits significant anti-nociceptive effects, making it a valuable tool for research in pain modulation and sensory neuron signaling. This compound is useful in investigations of neurogenic inflammation and the potential treatment of chronic pain conditions. -
TRPC Channel Inhibitor
ELP-004 is a selective TRPC channel inhibitor that targets TRPC-mediated calcium entry. It effectively inhibits osteoclast differentiation and activity, suppressing the translocation of NFATc1 in inflammatory osteoclastogenesis. Additionally, ELP-004 demonstrates a protective effect against bone erosion in mouse models of rheumatoid arthritis, making it a valuable tool for studying osteoclast biology and potential therapeutic strategies in bone degenerative diseases. -
TRPV4 Inhibitor
GSK2220691 is a potent antagonist of the transient receptor potential vanilloid 4 (TRPV4) channel. This compound effectively inhibits pulmonary edema induced by GSK1016790 and reduces HCl-induced increases in key mediators such as vascular endothelial growth factor (VEGF), keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF). GSK2220691 serves as a valuable tool for investigating TRPV4-related pathways and therapeutic applications in respiratory disorders. -
TRP Channel Agonist
4-(Phenyldiazenyl)benzoic acid is a selective TRP channel agonist that exhibits photosensitivity and photochemical switchability. This compound serves as a valuable pharmacological tool in the investigation of pain signaling pathways, offering researchers the ability to modulate TRPA1 activity through light exposure. Its unique properties make it suitable for studies focusing on nociception and sensory signaling mechanisms. -
TRPA1 Activator
Diisopropyl adipate is a TRPA1 activator that enhances FITC-induced contact hypersensitivity. This compound is utilized extensively as an alternative plasticizer in various formulations, serving not only as a key ingredient in cosmetic products but also as an excipient in pharmaceutical applications. By functioning as an emollient and plasticizer, diisopropyl adipate improves the stability, solubility, and overall processability of drug formulations, while influencing the absorption, distribution, metabolism, and elimination (ADME) characteristics of co-administered drugs. -
TRPV1 Antagonist
Oleoyl Serotonin is a TRPV1 antagonist, exhibiting an IC50 value of 2.57 μM for human TRPV1 receptors. This compound is implicated in the modulation of nociceptive pathways, making it a valuable tool for studies related to pain signaling and sensory transduction. Oleoyl Serotonin is suitable for research applications investigating inflammatory pain and potential therapeutic interventions targeting TRPV1. -
TRPV1 Agonist
MSP-3 is a potent agonist of the TRPV1 receptor, characterized by an EC50 of 0.87 μM. This compound demonstrates significant neuroprotective and antinociceptive properties, making it valuable for research focused on pain modulation and neuroprotection. Its ability to activate TRPV1 makes MSP-3 an important tool for investigating sensory physiology and related therapeutic interventions. -
TRP Channel Antagonist
TRPM8 Antagonist 3 is a selective antagonist targeting the Transient Receptor Potential Melastatin 8 (TRPM8) channel, exhibiting an IC50 value of 11 nM. This compound effectively inhibits TRPM8-mediated calcium influx, making it useful for studying nociceptive pathways and cold sensitivity. It has potential applications in research related to pain management, sensory biology, and neurobiology. -
TRPML1 Channel Antagonist/Microtubule Depolymerizer
Estradiol 3-methyl ether (EDME) is a potent antagonist of the TRPML1 ion channel and a microtubule depolymerizer. It exhibits remarkable selectivity, with IC50 values of 0.22 μM against TRPML1 and 3.8 μM against TRPML2, while showing no activity towards TRPML3. EDME disrupts cytoplasmic microtubule networks in mammalian cells with an EC50 of 9 μM. This compound operates independently of estrogen receptors to block autophagy, inhibit TFEB nuclear translocation, and reduce migration and invasion in triple-negative breast cancer cells, making it highly relevant for research in cancer biology. -
TRPV1 Receptor Activator
Phenylcapsaicin is a TRPV1 receptor activator known for its role in enhancing fat oxidation during aerobic exercise. This compound serves as an analogue of capsaicin, demonstrating similar biological activity. Its research applications are particularly relevant in studies focused on metabolic processes and pain modulation, providing insights into the physiological effects of TRPV1 activation. -
TRPM3 Activator
D-erythro-Sphingosine hydrochloride is a specific activator of the TRPM3 ion channel. This compound has been shown to induce dephosphorylation of the retinoblastoma protein, which can play a significant role in cell cycle regulation. D-erythro-Sphingosine hydrochloride is utilized in research focused on exploring TRPM3-related pathways and cellular processes. -
Stable Isotope
Resolvin D2-d5 is a deuterium-labeled derivative of Resolvin D2, a metabolite of docosahexaenoic acid (DHA). This compound exhibits significant anti-inflammatory and anti-infective properties, primarily by regulating leukocyte activity and modulating responses to microbial sepsis. Additionally, Resolvin D2 serves as a potent inhibitor of TRPV1 and TRPA1 channels in primary sensory neurons, with IC50 values of 0.1 nM and 2 nM, respectively. It is valuable for research applications focusing on inflammatory responses and pain pathways. -
TRPV1 Antagonist
ABT-102 is a potent and highly selective antagonist of the Transient Receptor Potential Vanilloid 1 (TRPV1) channel. This compound effectively elevates heat pain thresholds and diminishes the perception of pain in response to suprathreshold heat stimuli. ABT-102 has demonstrated efficacy in reducing nociceptive responses in various animal models, including those simulating inflammatory pain, bone cancer pain, postoperative pain, and osteoarthritis. -
TRPM8 Receptor Agonist
FEMA 4809 is a potent agonist of the TRPM8 receptor, with an EC50 of 0.2 nM. This compound is known for its ability to induce a cooling sensation through the activation of the TRPM8 ion channel, which is crucial for thermosensation. It is primarily utilized in research exploring thermal perception and related sensory pathways. -
TRPV4 Inhibitor
TRPV4-IN-5 is a selective TRPV4 inhibitor with an IC50 value of 0.46 μM. This compound exhibits significant efficacy in reducing acute lung injury symptoms induced by lipopolysaccharide in murine models. TRPV4-IN-5 is valuable for research into the modulation of TRPV4-associated pathways and potential therapeutic applications in lung inflammatory conditions. -
TRP Channel Inhibitor
Cannabidiorcol (CBDO) is an inhibitor of transient receptor potential (TRP) channels. This compound, structurally related to cannabidiol with a shortened pentyl side chain, exhibits anti-inflammatory properties while displaying low affinity for cannabinoid receptors. Research applications include investigations into its potential role in modulating inflammation and exploring its effects on tumorigenesis at elevated concentrations. -
TRPM8 Antagonist
Voacangine is a selective antagonist of the TRPM8 channel, competitively inhibiting the binding of menthol (IC50=9 μM) and noncompetitively inhibiting icilin (IC50=7 μM). It is known to block capsaicin binding to TRPV1 (IC50=50 μM) while exhibiting agonistic effects on TRPA1 (EC50=8 μM). Voacangine effectively antagonizes chemical agonist-induced activation of TRPM8, with no impact on cold-induced activation, making it a valuable tool for studying sensory signaling pathways. This alkaloid is derived from the root bark of Voacanga africana, providing a natural source for research applications. -
TRPV1 Antagonist
L-R4W2 is a potent antagonist of the vanilloid receptor 1 (VR1, TRPV1), exhibiting an IC50 of 0.1 μM. This compound demonstrates significant analgesic properties, making it a valuable tool in pain management research. L-R4W2 can be utilized to explore mechanisms of pain signaling and the therapeutic potential for treating pain-related disorders. -
TRPV1 Agonist
Vocacapsaicin is a first-in-class proagent of Capsaicin that targets the TRPV1 receptor as an agonist. This compound is known for its significant and enduring analgesic properties, making it a valuable tool in pain research. It is applicable in studies exploring non-opioid pain relief mechanisms and the modulation of sensory pathways. -
TRPV1 Agonist
Dihydrocapsiate is an orally active TRPV1 agonist derived from the capsinoid family. This compound stimulates the TRPV1 receptor, playing a significant role in thermogenesis and energy metabolism. Dihydrocapsiate is valuable for research applications related to metabolic diseases, providing insights into obesity, energy expenditure, and related disorders. -
TRPV1 Agonist
Vocacapsaicin hydrochloride is a potent TRPV1 agonist and a proagent of Capsaicin. This compound is primarily utilized in pain research, demonstrating significant and prolonged analgesic effects. Its unique mechanism offers valuable insights into non-opioid pain relief pathways, making it an important reagent for studies focused on pain modulation and sensory signaling. -
TRPA1 Agonist
TRPA1 Agonist-3 is a selective agonist for the TRPA1 ion channel, displaying EC50 values of 50.05 μM for human TRPA1 and 314.04 μM for mouse TRPA1. This compound does not activate other transient receptor potential channels, including hTRPV1 and hTRPM8. TRPA1 Agonist-3 has demonstrated efficacy in alleviating inflammatory pain in mouse models, operating through a channel desensitization mechanism, making it a valuable tool for studying pain pathways and TRPA1-related pharmacology. -
TRPV6 Inhibitor
TRPV6-IN-1 is a potent and selective inhibitor of the transient receptor potential cation channel subfamily V member 6 (TRPV6). It exhibits significant anti-proliferative effects, making it a valuable tool for cancer research. This compound can be utilized in studies investigating the role of TRPV6 in tumor growth and progression, aiding in the development of potential therapeutic strategies. -
FAAH Inhibitor and TRPV1 Antagonist
N-Arachidonoylserotonin is a potent fatty acid amide hydrolase (FAAH) inhibitor, exhibiting an IC50 value ranging from 1 to 12 µM. Additionally, it serves as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels, with an IC50 of 70 to 100 nM. Due to its dual action, N-Arachidonoylserotonin demonstrates significant analgesic properties in rodent models, making it a valuable tool for research in pain mechanisms and therapeutic interventions. -
TRPV1 Antagonist
AMG 7905 is a selective antagonist of the transient receptor potential vanilloid type 1 (TRPV1), known for its role in mediating pain and thermoregulation. This compound effectively inhibits TRPV1 channel activation by capsaicin while enhancing channel activation by protons. AMG 7905 is employed in research focusing on pain modulation, thermogenesis inhibition, and the physiological responses to temperature changes. -
TRPA1 Activator
Wasabi Receptor Toxin is an activator of the TRPA1 ion channel, functioning at nanomolar concentrations (EC50). This cell-penetrating scorpion toxin enhances the open time of TRPA1 while concurrently reducing calcium permeability. Its application in research includes the investigation of thermal hypersensitivity and mechanical allodynia in animal models, without inducing neurogenic inflammation. -
TRPC3 Agonist
OptoBI-1 is a photochromic agonist of the TRPC3 channel, functioning as a photopharmacological agent to modulate neuronal activity. This compound enables precise control of neuronal firing through light-induced conformational changes, facilitating studies in neural circuitry and synaptic transmission. OptoBI-1 is valuable for researchers investigating the role of TRPC3 in neurophysiology and related biological processes. -
TRPV1 Agonist
N-Linolenoylethanolamine (18:3 NAE) is a TRPV1 agonist that functions as an endocannabinoid. This compound is known to modulate pain and inflammatory responses through its interaction with the transient receptor potential vanilloid 1. It is valuable in research applications focused on neurobiology, pain management, and the endocannabinoid system. -
TRPV1 Antagonist
(S)-ABT-102 is a selective TRPV1 antagonist with an IC50 of 123 nM. It exhibits significant analgesic activity, making it a valuable tool for exploring pain pathways. This compound is utilized in research applications focused on pain management and the study of nociception mechanisms. -
TRP Channel Antagonist
TRPA1-IN-1 is a selective antagonist of the TRPA1 channel, exhibiting potent inhibitory effects on this target. This small molecule demonstrates oral bioavailability, making it suitable for in vivo studies. TRPA1-IN-1 is valuable for investigating the role of TRPA1 in pain signaling and inflammatory responses, contributing to research in neurobiology and pharmacology. -
TRPM3 Inhibitor
Ponometrep is a potent antagonist of the transient receptor potential melastatin 3 (TRPM3) channel, exhibiting IC50 values in the range of 1-10 nM. This compound demonstrates significant analgesic activity, making it a valuable tool for the study of pain mechanisms and neurological disorders. Its specificity for TRPM3 allows researchers to explore potential therapeutic applications in related biological pathways. -
TRP Channel Agonist
TRPV4 agonist-1 is a selective agonist of the transient receptor potential vanilloid 4 (TRPV4) channel, exhibiting an EC50 of 60 nM in human TRPV4 calcium assays. This compound is primarily utilized in research to investigate TRPV4-mediated pathways, including physiological functions like osmosensation and nociception. Its ability to activate TRPV4 makes it valuable for studying various biological processes and potential therapeutic applications related to TRP channels. -
TRPV1 Antagonist
V116517 is a potent orally active antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It effectively inhibits capsaicin- and acid-induced currents in rat dorsal root ganglion neurons expressing native TRPV, with IC50 values of 423.2 nM for capsaicin and 180.3 nM for acid. This compound is valuable for research related to pain mechanisms and potential therapeutic interventions. -
Photoswitchable Diacylglycerol
18:0-PhoDAG is a photoswitchable diacylglycerol (DAG) that enables precise photoactivation of DAG-sensitive transient receptor potential (TRP) channels. This compound serves as a valuable tool in elucidating the signaling pathways associated with TRP channel activity in various biological systems. Its use in photopharmacology facilitates real-time studies of cellular responses to DAG modulation, enhancing understanding of cellular signal transduction phenomena. -
TRPA1 Agonist
Methyl kakuol is a selective agonist of the transient receptor potential ankyrin 1 (TRPA1) channel, exhibiting an effective concentration (EC50) of 0.27 µM. This compound facilitates the activation of TRPA1, making it a valuable tool for research into sensory pathways and pain mechanisms. Its ability to modulate TRPA1 activity can aid in the exploration of neurophysiological responses and the development of therapeutic strategies targeting pain and inflammation. -
TRPV1 Agonist
Polygodial pyridazine is a TRPV1 agonist that exhibits a GI50 of 72 μM against MCF-7 cancer cell lines. This compound is a polygodial analogue that plays a crucial role in exploring the mechanisms of pain perception and inflammation. It is applicable for research focused on cancer biology and the modulation of sensory neuronal pathways. -
TRPM7 Inhibitor
AAL-149 is a selective inhibitor of the TRPM7 ion channel, exhibiting an IC50 value of 1.081 μM. This compound demonstrates multimodal anti-inflammatory effects while avoiding interaction with sphingosine-1-phosphate (S1P) receptors. AAL-149 is a valuable tool for researchers investigating the role of TRPM7 in inflammation and related biological pathways. -
TRPV4 Antagonist
TRPV4 antagonist 4 is a selective TRPV4 antagonist with an IC50 value of 22.65 nM, effectively inhibiting TRPV4-mediated ion currents. This compound demonstrates protective effects in models of acute lung injury, making it a valuable tool for research focused on respiratory diseases and cellular calcium signaling. Its specificity for the TRPV4 channel highlights its potential in studying TRPV4-related physiological and pathological processes. -
TRP Channel Antagonist
AMG0347 is a potent antagonist of the transient receptor potential type V1 (TRPV1) channel. It effectively inhibits TRPV1 activation by heat (IC50 = 0.2 nM), protons (IC50 = 0.8 nM), and capsaicin (IC50 = 0.7 nM). This compound is useful for research applications related to nociception, pain pathways, and sensory neuron function. -
TRPV1 Modulator
AMG-8562 is a selective modulator of the TRPV1 ion channel, effectively inhibiting capsaicin activation while sparing heat-induced activation. This compound enhances TRPV1 activation at acidic pH levels and demonstrates significant analgesic properties by blocking capsaicin-induced flinching behaviors in various pain models. AMG-8562 has shown substantial efficacy in models of thermal hyperalgesia induced by complete Freund's adjuvant and skin incision, as well as in acetic acid-induced writhing assays, making it a valuable tool for pain research. -
TRPM8 Receptor Agonist
TRPM8 receptor agonist-1 is a selective agonist for the TRPM8 receptor, known for its ability to induce the inward flow of calcium, sodium, and other ions, resulting in cell membrane depolarization and subsequent action potential generation. This compound plays a crucial role in activating pathways associated with the swallowing reflex, making it valuable for research on oropharyngeal dysphagia and related conditions. Its activation of TRPM8 receptors positions it as a significant tool for exploring ion channel dynamics and therapeutic approaches in dysphagic disorders. -
TRPV1 Antagonist
JTS-653 is a potent and selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It demonstrates significant efficacy in attenuating chronic pain that is resistant to non-steroidal anti-inflammatory medications. This compound is valuable for research into pain management and the mechanisms underlying TRPV1-related conditions. -
TRPV1 Antagonist
6-Iodonordihydrocapsaicin is a selective antagonist of the TRPV1 receptor. It effectively inhibits TRPV1-mediated responses, such as capsaicin-induced ion currents in dorsal root ganglion neurons and the distension-induced firing of jejunal spinal afferent fibers in murine models. This compound is valuable for research focused on visceral pain mechanisms and the exploration of anxiety disorders. -
TRPV4-KCa2.3 Protein Complex Enhancer
TRPV4-KCa2.3 modulator 1 is a modulator that enhances the TRPV4-KCa2.3 protein complex, exhibiting significant antihypertensive activity. This compound promotes hyperpolarization and vasodilation in endothelial cells. Its ability to influence vascular responses makes it a valuable tool for investigating hypertension and related cardiovascular disorders in research settings. -
TRPM2 Inhibitor
TRPM2-IN-1 is a selective inhibitor of the TRPM2 ion channel, which plays a critical role in calcium influx and cellular signaling. This compound has demonstrated significant neuroprotective effects and exhibits antistroke activity, making it a valuable tool in the study of ischemic stroke and related neurological disorders. Its capacity to modulate TRPM2 activity provides insight into potential therapeutic strategies for neurodegenerative conditions. -
TRP Channel Inhibitor
HZS60 is a selective TRP channel inhibitor that demonstrates significant neuroprotective effects against cerebral ischemia. It effectively mitigates primary neuronal damage induced by NMDA and oxygen-glucose deprivation/reoxygenation. Additionally, HZS60 exhibits favorable pharmacokinetic properties and can reduce injury associated with cerebral ischemia-reperfusion. This compound serves as a promising candidate for research applications targeting ischemic stroke. -
TRPC Antagonist
TRPC Antagonist 1 is a potent antagonist of transient receptor potential channels, specifically targeting TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7, with IC50 values of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM, respectively. This compound exhibits significant anti-glioblastoma activity in vitro, effectively inhibiting the proliferation of U87 cell lines. It serves as a valuable tool for exploring the role of TRPC channels in various biological processes and disease models. -
TRPV1 Agonist
Capsiconiate, a TRPV1 agonist, exhibits a potent efficacy with an EC50 of 3.2 μM. This compound serves as a valuable tool for investigating TRPV1-mediated conditions, including pain, inflammation, and epilepsy. Its ability to activate the TRPV1 receptor makes it significant in the study of related pathophysiological mechanisms and therapeutic interventions. -
TRP Channel Agonist
AMG 9090 is a partial agonist of the rat TRPA1 channel, exhibiting significant pharmacological activity in models of pain and inflammation. TRPA1 plays a critical role in detecting reactive compounds that induce pain responses in both humans and rodents. Notably, AMG 9090 demonstrates a distinct antagonistic effect on human TRPA1 activated by AITC and noxious cold, while functioning as a partial agonist in rat TRPA1. This profile highlights the compound’s potential utility as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory effects observed on TRPM8 channels. -
TRPV1 Inhibitor
TRPV1-IN-3 is a selective inhibitor of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating significant antifibrotic activity in vitro with an IC50 of 0.51 μM. Its mechanism involves the modulation of fibrosis markers such as collagen I and α-SMA through inhibition of the TGF-β/Smads and MAPK signaling pathways. Research applications include studying idiopathic pulmonary fibrosis, where TRPV1-IN-3 has been shown to reduce collagen deposition in lung tissue, enhance alveolar structure, and increase survival rates in Bleomycin-induced pulmonary fibrosis models.
