Catalog No.
Product Name
Application
Product Information
Citations
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TRPC4/5 Inhibitor
TRPC4/5-IN-3 is a potent inhibitor of the transient receptor potential canonical channels 4 and 5, exhibiting IC50 values of 3.6 nM and 5.5 nM, respectively. This compound shows additional hERG channel inhibition with an IC50 of 6.5 µM, along with favorable metabolic stability in liver microsomes from humans, rats, and mice. TRPC4/5-IN-3 demonstrates significant antidepressant and anxiolytic effects in murine models and possesses excellent pharmacokinetic properties, highlighted by an oral bioavailability of 87%. This reagent is valuable for research involving TRPC channel modulation and related therapeutic pathways. -
TRPC3/6 Blocker
TRPC3/6-IN-3 is a selective inhibitor of TRPC3 and TRPC6 channels, primarily targeting the regulation of calcium influx in cells. This compound exhibits significant biological activity in modulating vascular smooth muscle contraction and endothelial function, making it relevant for cardiovascular disease research. TRPC3/6-IN-3 offers a valuable tool for elucidating the roles of these channels in various pathophysiological conditions, contributing to the understanding of cardiovascular mechanisms. -
TRP Channel Antagonist
TRPV4 antagonist 3 is a selective antagonist of the TRPV4 ion channel, demonstrating a pIC50 value of 8.4. This compound effectively inhibits TRPV4-mediated calcium influx, making it a valuable tool for investigating the physiological roles of TRPV4 in various biological processes. It has potential applications in pain research, inflammation studies, and the exploration of therapeutic strategies for TRPV4-related disorders. -
TRPA1 Antagonist
ZQMT-10 is a potent and orally active antagonist of the transient receptor potential ankyrin 1 (TRPA1), exhibiting a Kd of 1.04 μM. This compound is significant in cancer research, offering insights into the mechanisms of pain and inflammation associated with tumor development. Its selective inhibition of TRPA1 makes it a valuable tool for understanding its role in various physiological and pathological processes. -
TRPM7 Inhibitor
BTB 06061 is a selective inhibitor of the TRPM7 ion channel, known for its involvement in cellular magnesium homeostasis and signaling. This compound exhibits significant biological activity in modulating TRPM7-mediated pathways, making it a valuable tool for investigating ischemic diseases and related conditions. Its application in research can enhance the understanding of TRPM7's role in cellular processes and disease mechanisms. -
rVR1 Modulator
KJM429 is a high-affinity ligand targeting the rat vanilloid receptor rTRPV1, exhibiting a Ki value of 30-63 nM. This compound functions as a competitive antagonist to inhibit TRPV1 activation by stimuli such as capsaicin, resiniferatoxin, and thermal signals, while switching to an agonist role under acidic conditions (pH < 5.5). KJM429 effectively modulates calcium influx associated with TRPV1 activation, making it a valuable tool for investigating the mechanisms underlying pain-related disorders, including postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis, and pruritus. -
TRPV1 Antagonist
MK-2295 (NGD-8243) is a potent TRPV1 antagonist that plays a crucial role in pain modulation. Its primary biological activity is as an analgesic agent, making it a valuable tool for research aimed at understanding and addressing pain mechanisms. MK-2295 is useful in studies exploring the therapeutic potential of TRPV1 inhibition in various pain-related conditions. -
TRPM2 Inhibitor
8-Br-ADPR (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor that antagonizes the ADPR signaling pathway. This compound inhibits glucagon-mediated nuclear calcium signaling and downstream signaling through CaMKII/CREB phosphorylation by preventing ADPR-induced activation of TRPM2. In diabetic models, 8-Br-ADPR effectively decreases gluconeogenic gene expression and lowers blood glucose levels. Additionally, it inhibits ADPR-mediated calcium signaling in NK cells, affecting immune synapse formation, granzyme B release, and cytolytic activity against melanoma cells. 8-Br-ADPR is useful in research on diabetes, melanoma, and lymphoma. -
TRPM2 Channel Inhibitor
ZA18 is a selective inhibitor of the TRPM2 channel, characterized by an IC50 value of 6.2 μM. This compound effectively mitigates intracellular calcium overload caused by TRPM2 activation and significantly decreases the mortality of SH-SY5Y cells subjected to H2O2-induced stress. ZA18 is suitable for investigating mechanisms underlying ischemia-reperfusion injury, inflammation, and various neurodegenerative diseases. -
TRPC5 Inhibitor
TRPC5-IN-3 is a selective inhibitor of the Transient Receptor Potential Cation Channel 5 (TRPC5), exhibiting an IC50 value of 10.75 nM. This compound has demonstrated significant potential in modulating calcium influx in cells and is useful for studying TRPC5-related physiological processes and pathologies. Its applications include investigating the role of TRPC5 in neurobiology, renal function, and various disease states. -
TRPA1 Inhibitor
GDC-0334 is a selective antagonist of the Transient Receptor Potential Ankyrin 1 (TRPA1) channel. It effectively inhibits TRPA1 function in airway smooth muscle and sensory neurons, leading to decreased cough reflex and reduced allergic airway inflammation in preclinical models. This compound is valuable for research focused on TRPA1-mediated conditions, including pain and asthma, facilitating the study of therapeutic interventions targeting these pathways. -
TRPC3 Agonist
TRPC3 agonist-1 is a selective and competitive agonist of the TRPC3 channel, acting primarily at the L2 binding site of human TRPC3. This compound enhances TRPC3 channel activity, making it valuable for research on calcium signaling pathways and related physiological processes. Its ability to modulate TRPC3 function can aid in investigations of various conditions, including neurological disorders and cardiovascular diseases. -
TRPV1 Antagonist
ABT-116 is an orally active antagonist of the transient receptor potential vanilloid type 1 (TRPV1) channel. This compound demonstrates significant analgesic efficacy, making it a valuable tool in pain research. ABT-116 is particularly relevant for studies focusing on neurological diseases and the modulation of pain pathways. -
TRPV1 Agonist
SA-13353 is a potent agonist of the TRPV1 receptor, known for its cardioprotective effects. This compound is instrumental in the study of cardiovascular diseases, facilitating research into mechanisms of cardiac protection and potential therapeutic interventions. Its ability to modulate TRPV1 activity makes it a valuable tool for investigating the role of this receptor in cardiovascular health. -
TRP Channel
AS1928370 is a selective antagonist of the TRPV1 ion channel, demonstrating the ability to inhibit ligand-induced activation in vivo. This CNS-penetrant compound is particularly valuable for studying mechanisms underlying neuropathic pain. Its application in research offers insights into pain modulation and potential therapeutic strategies for pain management. -
Stable Isotope
4-Methyl-2-(1-piperidinyl)-quinoline-d10 is a deuterated analogue of ML204, functioning as a selective inhibitor of the TRPC4 and TRPC5 ion channels. This compound exhibits a significant 19-fold selectivity over TRPC6 and has minimal impact on other TRP channels, as well as voltage-gated sodium, potassium, and calcium channels. It is a valuable tool for investigating TRPC channel functions and their roles in various biological processes. -
TRPV1 Antagonist
TRPV1 antagonist 5 is a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. This compound demonstrates potent inhibitory activity against TRPV1, making it a valuable tool for studies focused on pain signaling and thermoregulation. Research applications include investigating nociceptive pathways and exploring therapeutic potential for inflammatory pain relief. -
TRPV1 Agonist
TRPV1 agonist-1 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) channel, exhibiting EC50 values of 4.5 nM and 0.57 nM for human and rat TRPV1, respectively. This compound is effective in enhancing swallowing function in preclinical rat models, making it valuable for investigating dysphagia and related disorders. Its non-irritating profile allows for potential applications in functional studies involving TRPV1 modulation. -
TRPV1 Agonist
JYL-273 analog-1 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) ion channel, exhibiting a Ki value of 10.8 nM. This compound demonstrates significant analgesic activity, with an ED50 of 1.0 mg/kg in the PBQ-induced writhing test. JYL-273 analog-1 is suitable for investigations into pain mechanisms and the development of analgesic therapies. -
TRPM8 Antagonist
AMG8788 is a selective, orally active antagonist of the transient receptor potential melastatin 8 (TRPM8), exhibiting an IC50 of 63.2 nM. This compound demonstrates significant inhibitory activity on TRPM8, making it valuable for studying sensory perception, pain pathways, and thermoregulation. It serves as an important tool for research into conditions associated with TRPM8 modulation, including neuropathic pain and cold sensitivity. -
TRPC5 Inhibitor
TRPC5-IN-2 is a selective inhibitor of the transient receptor potential cation channel 5 (TRPC5), known for its role in calcium ion influx and various physiological processes. This compound has demonstrated significant inhibitory activity against TRPC5, making it valuable for research into calcium signaling and its implications in neurological disorders, cardiovascular diseases, and gene regulation. TRPC5-IN-2 is essential for studies aimed at elucidating the functional roles of TRPC5 and exploring potential therapeutic interventions. -
TRPM5 Agonist
TRPM5 agonist-1 is a potent TRPM5 agonist with a pEC50 of 8.1, demonstrating strong selectivity over related cation channels such as TRPM8, TRPV1, TRPV4, TRPA1, and TRPM4. This compound elicits a stimulatory effect on gastrointestinal transit in mouse models, making it valuable for studies focused on enhancing gastric motility. TRPM5 agonist-1 is suitable for research exploring the roles of TRPM5 in gastrointestinal physiology and motility regulation. -
TRPM8 Antagonist
AMG9678 is a selective, orally active antagonist of the transient receptor potential melastatin 8 (TRPM8) channel, exhibiting a potent inhibitory effect with an IC50 value of 31.2 nM. This compound is utilized in research focused on pain modulation, thermosensation, and neurogenic inflammation, providing insights into the role of TRPM8 in various physiological and pathological processes. Its specificity and potency make it a valuable tool for investigating TRPM8-related biological pathways. -
TRPV4/TRPA1 Inhibitor
TRPV4/TRPA1-IN-1 is a selective inhibitor of the TRPV4 and TRPA1 channels, effectively blocking calcium influx mediated by these targets. This compound demonstrates significant efficacy in reducing pain behaviors in mouse models, particularly in trigeminal stimulation and acute pancreatitis contexts. TRPV4/TRPA1-IN-1 is valuable for research focused on pain modulation and inflammation associated with acute pancreatitis. -
TRPV1 Channel Antagonist
JNJ-38893777 is a selective antagonist of the transient receptor potential vanilloid type 1 (TRPV1) channel. By inhibiting neuronal hyperactivation, JNJ-38893777 effectively reduces inflammatory hyperalgesia, making it a valuable tool for studies focused on migraine headaches, as well as neuropathic and inflammatory pain research. Its oral activity further enhances its potential in pharmacological applications targeting pain modulation. -
Capsaicin Analog
TRPV1 activator-1 is a capsaicin analog with a modified neck structure that specifically interacts with the T551 residue of the TRPV1 receptor. This compound is known for its ability to activate TRPV1, contributing to research on pain sensation and nociception. Its unique properties make it a valuable tool for studying the physiological and pharmacological aspects of TRPV1-mediated pathways in various pain-related studies. -
Capsaicin Analog
TRPV1 activator-2 is a capsaicin analog that specifically targets the TRPV1 ion channel, enhancing its activity in response to thermal and chemical stimuli. This compound is utilized in research to study pain signaling pathways, neuroinflammation, and the physiological effects of TRPV1 modulation. Its precise interactions with channel residues at the lipid-water interface contribute to a better understanding of TRPV1's role in nociception and potential therapeutic applications. -
Analgesic Agent
Davasaicin is a derivative of capsaicin and functions as an orally active analgesic agent. It is primarily used for the management of pain through its interaction with TRPV1 receptors, leading to altered pain signaling pathways. This compound serves as a valuable tool for research focused on pain mechanisms and potential therapeutic interventions in acute and chronic pain conditions. -
TRPM2 Agonist
(E/Z)-Farnesyl pyrophosphate is a 15-carbon isoprenoid that acts as a TRPM2 agonist, facilitating ion influx through the channel. As a critical metabolic intermediate of the mevalonate pathway, it plays a significant role in cholesterol synthesis, ubiquinones synthesis, and protein farnesylation. This compound is essential for research in cellular signaling and lipid metabolism, providing insights into various biological processes and potential therapeutic targets. -
TRPM8 Antagonist
DFL23448 is a selective antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. It demonstrates potent inhibition with IC50 values of 10 nM and 21 nM in human embryonic kidney 293 cells stimulated by Cooling Agent 10 or cold exposure. DFL23448 exhibits minimal activity against other transient receptor potential channels, such as TRPV1, TRPA1, and TRPV4, as well as various G protein-coupled receptors. This compound has potential applications in modifying bladder function and alleviating bladder overactivity in in vivo models. -
TRPV1 Agonist
Linopirdine dihydrochloride is an agonist of the capsaicin receptor TRPV1, which plays a key role in nociception. This compound enhances intracellular calcium levels in HEK293 cells, leading to increased excitatory responses in mammalian nociceptors. Linopirdine dihydrochloride is valuable for research applications focused on pain mechanisms and sensory neuron function. -
TRPV1 Agonist
JYL-273 is a potent TRPV1 agonist, exhibiting an IC50 of 361 nM in CHO-TRPV1 cell lines. This compound is useful for studying pain mechanisms and sensory neuron activation, making it a valuable tool in pain research and neurobiology. Its ability to selectively activate TRPV1 can aid in the investigation of pain pathways and the development of analgesic therapies. -
TRPV2 Channel Inhibitor
Murpanicin is a coumarin compound that functions as a selective inhibitor of the thermosensitive transient receptor potential vanilloid 2 (TRPV2) channel. Its potent anti-inflammatory properties make it a valuable tool for studying inflammation pathways, while its insecticidal effects allow for exploration in entomological research. This compound offers potential applications in the development of therapeutic agents targeting TRPV2-mediated processes. -
TRPV1 Antagonist
SAR-115740 is a TRPV1 antagonist that selectively inhibits the transient receptor potential vanilloid 1 channel. This compound has demonstrated developmental toxicity in H9 cell assays, highlighting its potential impact on cellular differentiation and viability. SAR-115740 is valuable for investigating inflammatory conditions and neurological disorders, contributing to research aimed at understanding pain mechanisms and developing therapeutic strategies. -
TRPV1 Desensitizing Agent
Palvanil is a potent TRPV1 desensitizing agent, acting as an analogue of Capsaicin. It exhibits significant anti-nociceptive and anti-inflammatory properties, making it a valuable tool in pain research. Palvanil's mechanism of action provides insights into the modulation of TRPV1 receptor activity, facilitating studies on pain and inflammatory pathways. -
TRPV1 Antagonist
AZ12099548 is a selective antagonist of the TRPV1 receptor, which plays a critical role in pain and sensory perception. This compound effectively inhibits calcium mobilization induced by both capsaicin and low pH, making it a valuable tool for research into pain mechanisms and sensory disorders. Its utility in studying TRPV1-related pathways facilitates investigations into potential therapeutic strategies for inflammatory and neuropathic pain conditions. -
TRPC5 Inhibitor
TRPC5-IN-4 is a potent inhibitor of the TRPC5 channel, with an IC50 value of 14.07 nM for TRPC5 and 65 nM for TRPC4. This compound demonstrates minimal cytotoxicity, exhibiting no detrimental effects on liver and kidney cells. TRPC5-IN-4 is particularly valuable for investigating mechanisms underlying chronic kidney disease (CKD) and holds potential for supportive research in this area. -
TRPC3/TRPC6 Antagonist
GSK2332255B is a highly selective antagonist of TRPC3 and TRPC6 channels, exhibiting IC50 values of 5 nM and 4 nM, respectively, for rat TRPC3 and TRPC6. This compound demonstrates over 100-fold selectivity for TRPC3 and TRPC6 compared to other calcium-permeable channels. GSK2332255B is valuable for research applications investigating the role of TRPC channels in various physiological and pathological processes. -
TRPV1 Activator
RhTx is a transient receptor potential vanilloid 1 (TRPV1) activator that plays a crucial role in the modulation of pain perception. By enhancing TRPV1 activity, RhTx facilitates research into pain mechanisms and is valuable for studying nociception and the sensory transduction processes involved in inflammatory pain responses. This compound serves as a useful tool in pain research and therapeutic studies targeting TRPV1-related pathways. -
TRPV1 Antagonist
BCTP is a selective antagonist of the TRPV1 receptor, functioning through inhibition of ion channel activity. It exhibits potent antagonistic effects on human TRPV1 in CHO cells, with an IC50 of 18 nM at low pH conditions. BCTP is valuable for research into mechanisms underlying chronic pain and can aid investigations into pain modulation pathways. -
TRP Channel Inhibitor
Resolvin D2 methyl ester is a methyl ester derivative of the docosahexaenoic acid metabolite Resolvin D2, functioning as a TRP channel inhibitor. It exhibits significant anti-inflammatory and anti-infective properties, effectively modulating leukocyte activity. The compound selectively inhibits neuronal TRPV1 (IC50=0.1 nM) and TRPA1 (IC50=2 nM), making it a valuable tool in sepsis research and related studies on inflammation. -
TRPV1 Channel Antagonist
TRPV1 antagonist 9 is a potent antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It effectively inhibits calcium influx in Chinese hamster ovary (CHO) cells expressing TRPV1 receptors, with IC50 values of 0.6 nM for capsaicin and 0.8 nM for acid-induced calcium uptake. This compound has demonstrated the ability to block capsaicin-induced flinch responses and can induce hyperthermia in rat models, making it a valuable tool for exploring nociceptive pathways and pain mechanisms. -
TRPV4 Antagonist
HC-067047 hydrochloride is a potent and selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4). It effectively inhibits TRPV4 currents in human, rat, and mouse orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively. This compound is valuable for research into TRPV4-related physiological processes and the development of therapeutic strategies targeting this ion channel. -
TRPV3 Receptor Antagonist
N-Oleoyl valine is a N-acyl valine derivative that functions as an antagonist of the TRPV3 receptor. This compound exhibits significant biological activity in modulating thermal and pain sensation, making it valuable for research in pain management and sensory biology. It is used in studies investigating the mechanisms of TRPV3-mediated signaling pathways and potential therapeutic targets in sensory disorders. -
TRPV4 Channel Activaitor
Bisandrographolide A is a potent TRPV4 channel activator with an EC50 ranging from 790 to 950 nM. This compound has demonstrated anti-inflammatory, immunostimulant, and antihypertensive properties. Additionally, Bisandrographolide A binds to CD81, leading to functional suppression, making it valuable for research applications in inflammation, immune response, and cardiovascular studies. -
TRPV1 Antagonist
(Rac)-AMG 628 is a potent TRPV1 antagonist, exhibiting an IC50 of 3.7 nM. This compound is valuable for research in chronic pain mechanisms, providing insights into the role of TRPV1 in nociception and pain modulation. Its efficacy makes it a noteworthy tool for exploring potential therapeutic avenues in pain management. -
TRPM2 Channel Agonist
2′-Deoxy-ADPR is an agonist of the transient receptor potential melastatin 2 (TRPM2) channel. This compound is involved in calcium signaling within cells, particularly in Jurkat T-lymphocytes, where it plays a critical role in mediating cellular responses. 2′-Deoxy-ADPR is valuable for research investigating the effects of TRPM2 activation in various physiological and pathological processes. -
TRPM2 Antagonist
8-Br-7-CH-ADPR, a specific TRPM2 antagonist, effectively inhibits TRPM2 activation by binding to the NUDT9 homology domain of the TRPM2 channel. This modulation controls cation influx through the cell membrane, making it a valuable tool for investigating the physiological and pathological roles of TRPM2. Applications include studying cell death, neurodegenerative diseases, myocardial infarction, and diabetes, providing insights into TRPM2's involvement in various biological processes. -
TRPV1 Antagonist
(S)-AMG-628 is a selective TRPV1 antagonist that effectively inhibits capsaicin- and acid-induced calcium influx, demonstrating IC50 values of 7 nM and 5 nM, respectively, in CHO cells. This compound has shown significant efficacy in reducing capsaicin-induced flinching behavior in rats and reversing thermal hypersensitivity in CFA-induced inflammatory pain models. As such, (S)-AMG-628 serves as a valuable tool in research addressing pain mechanisms and potential therapeutic interventions for inflammatory pain conditions.
