Catalog No.
Product Name
Application
Product Information
Citations
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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. -
TRP Channel
TRPC6-IN-2 is a selective inhibitor of TRPC6 channels. This compound effectively inhibits TRPC6 protein activity, making it a valuable tool for studying calcium signaling pathways. TRPC6-IN-2 can be utilized in various research applications, including investigations into cardiovascular and neurological disorders where TRPC6 plays a critical role in cellular function. -
TRP Channel Agonist
TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist designed to facilitate optical control of the TRPA1 channel. This compound allows for precise modulation of TRPA1 activity, making it an essential tool for research in sensory physiology and nociception. Its unique properties enable researchers to investigate the roles of TRPA1 in pain pathways and other physiological processes with enhanced spatial and temporal resolution. -
TRPM4 Antagonist
CMP233 is a potent TRPM4 antagonist with an IC50 value of 0.15 μM. This compound is valuable in the study of neurodegenerative disorders, providing insights into the role of TRPM4 channels in various pathological conditions. Its high specificity and efficacy make it a key tool for researchers investigating TRPM4-mediated signaling pathways. -
TRPC3/6 Inhibitor
TRPC3/6-IN-2 is a potent inhibitor targeting the TRPC3 and TRPC6 channels, exhibiting IC50 values of 16 nM and 29.8 nM for TRPC3 and TRPC6, respectively. This compound is valuable for investigating the physiological and pathological roles of TRPC channels in various cellular processes. It can be utilized in research focused on cardiovascular function, neuronal signaling, and other conditions associated with TRPC dysregulation. -
TRPV Antagonist
AMG8163 is an orally active antagonist of the TRPV1 receptor. This compound effectively inhibits capsaicin-induced flinching in rat models, demonstrating significant anti-hyperalgesic properties across various pain models. AMG8163 serves as a valuable tool for research focused on pain mechanisms and potential therapeutic interventions for hyperalgesia. -
TRPV4 Antagonist
RN-9893 hydrochloride is a potent antagonist of the transient receptor potential vanilloid 4 (TRPV4) channel, exhibiting IC50 values of 0.42 μM for human and 0.66 μM for rat TRPV4. This compound is valuable for research focused on TRPV4-related physiological processes and pathologies, including pain sensation and inflammatory responses. Its oral bioactivity makes it suitable for in vivo studies investigating the role of TRPV4 in various biological systems. -
TRPC5 Inhibtior
TRPC5-IN-5 is a selective inhibitor of the Transient Receptor Potential Canonical 5 (TRPC5), with an IC50 value of 1.28 μM. This compound exhibits promising biological activity, making it valuable for research focused on neurological and renal diseases. Its ability to modulate TRPC5 activity provides insights into potential therapeutic strategies for disorders associated with these systems. -
TRP Channel Activator
AM12 is a selective TRP channel activator that specifically inhibits Lanthanide-evoked TRPC5 activity, demonstrating an IC50 value of 0.28 μM. This compound is valuable for research investigating the modulation of TRPC5 channels and their role in calcium signaling pathways. AM12 is ideal for studies focused on cellular responses to TRP channel activation and the physiological implications in various biological systems. -
TRPC4/5 Inhibitor
TRPC4/5-IN-1 is a selective inhibitor of the transient receptor potential channel 4 and 5 (TRPC4/5), exhibiting IC50 values of 2.06 μM and 0.54 μM, respectively. This compound demonstrates significant biological activity in modulating TRPC channel-mediated calcium influx, making it useful for investigations into proteinuric kidney diseases and skin inflammatory conditions. Its targeted inhibition offers potential insights into the underlying mechanisms of these pathologies and may aid in the development of novel therapeutic strategies. -
Natural Product
Bisandrographolide C is a natural product derived from the plant Andrographis paniculata, characterized as a dimer of ent-labdane diterpenoid. This compound is known to activate TRPV1 and TRPV3 channels, exhibiting Kd values of 289 μM and 341 μM, respectively. Its biological activity includes cardioprotective effects against hypoxia-reoxygenation injury, making it a valuable reagent for research in molecular and cardiovascular studies. -
TRPC5 Modulator
TRPC5 modulator-1 is a potent modulator of the TRPC5 ion channel, demonstrating an IC50 of less than 1 nM. This compound is primarily utilized in research focused on neuropsychiatric disorders, providing insights into the mechanisms underlying these conditions. The modulation of TRPC5 may offer potential therapeutic strategies for addressing various neurological and psychiatric disorders. -
ACU Inhibitor/VR1 Agonist
OMDM-5 is a selective anandamide cellular uptake (ACU) inhibitor, exhibiting a Ki of 4.8 μM. In addition, OMDM-5 demonstrates potent activity as a vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM. This compound also shows weak activity as a cannabinoid receptor type 1 (CB1) ligand, with a Ki of 4.9 μM. Its properties make OMDM-5 useful for studies involving pain modulation and endocannabinoid signaling pathways.
