Catalog No.
Product Name
Application
Product Information
Citations
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TRPV1 Receptor Agonist
Olvanil (NE-19550) is a potent agonist of the transient receptor potential vanilloid type 1 (TRPV1) receptor, exhibiting an EC50 of 0.7 nM. This compound demonstrates analgesic properties and is valuable for investigating pain pathways and inflammatory responses. It is suitable for research applications focused on nociception and related signaling mechanisms. -
TRPA1 Inhibitor
AP-18 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1), effectively blocking TRPA1 activation by 50 µM cinnamaldehyde with IC50 values of 3.1 µM for human and 4.5 µM for mouse TRPA1. This compound demonstrates significant analgesic properties, as it reverses complete Freund's adjuvant-induced mechanical hyperalgesia in murine models. Additionally, AP-18 significantly reduces AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 µM, making it a valuable tool for research into pain mechanisms and TRPA1-related pathways. -
TRPM7 Inhibitor
VPC01091.4 is a potent TRPM7 inhibitor that effectively blocks TRPM7 current at low micromolar concentrations. This compound is capable of crossing the blood-brain barrier, making it suitable for neurological studies. Additionally, VPC01091.4 demonstrates significant anti-inflammatory properties, halting systemic inflammation in vivo, and can be utilized in research focused on inflammation and neuronal signaling pathways. -
TRPV3 Antagonist
TRPV3 antagonist 74a is a selective and potent inhibitor of the transient receptor potential vanilloid 3 (TRPV3) channel. Exhibiting minimal activity against a broad range of other ion channels, this compound serves as a valuable tool for investigating the role of TRPV3 in various biological processes. Its specific antagonistic properties make TRPV3 antagonist 74a particularly useful in research focusing on neuropathic pain and related disorders. -
TRP Channel Antagonist
Asivatrep (PAC-14028) is a potent and selective antagonist of the transient receptor potential vanilloid type I (TRPV1) channel. This compound exhibits significant analgesic effects by blocking TRPV1, which is involved in the transmission of nociceptive signals. Asivatrep is primarily utilized in research related to pain management and neurobiology. Its selective inhibition offers a valuable tool for studying TRPV1-mediated pathways and their role in various physiological and pathological conditions. -
TRPA1 Inhibitor
BAY-390 is a selective TRPA1 inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent inhibitory activity with IC50 values of 16 nM for human TRPA1 (hTRPA1) FLIPR, 82 nM for hTRPA1 electrophysiology (Ephys), 63 nM for rat TRPA1 (rTRPA1) FLIPR, and 35 nM for rat dorsal root ganglion (DRG) Ephys. BAY-390 is suitable for investigating the role of TRPA1 in inflammation-related research. -
TRPA1 Inhibitor
Nedizantrep is a potent inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel, demonstrating IC50 values of 5.3 nM in humans and varying efficacy across different species. This compound is utilized in research focused on neuropathic pain and respiratory conditions, including asthma and chronic cough. Its selective action on TRPA1 underscores its potential as a valuable tool for advancing studies aimed at understanding and treating these conditions. -
TRP Channel Agonist
D-3263 hydrochloride is a selective agonist of the transient receptor potential melastatin member 8 (TRPM8) channel. This compound exhibits key biological activity by modulating nociceptive signaling pathways, which are involved in pain perception and temperature regulation. It is primarily utilized in research related to pain management, sensory neuronal activity, and the physiological responses to cold stimuli. -
TRPC6 Inhibitor
Apecotrep is a potent inhibitor of the transient receptor potential C6 (TRPC6) ion channel. This orally active compound effectively modulates intracellular calcium levels and influences membrane potential by regulating the flux of calcium and sodium ions. Apecotrep is particularly relevant for research involving the respiratory system, providing insights into the role of TRPC6 in various biological processes. -
TRP Channel Agonist
TRPV4 agonist-1 free base is a selective agonist of the transient receptor potential vanilloid 4 (TRPV4) channel, demonstrating an EC50 of 60 nM in human TRPV4 calcium assays. This compound induces calcium influx and is instrumental in studies focused on the physiological roles of TRPV4 in nociception, osmoregulation, and cellular mechanotransduction. Research applications include investigating the channel's involvement in pain pathways and potential therapeutic targets for related disorders. -
TRPML2/3 Activator
(1S,2S)-ML-SI3 is a selective activator of the TRPML2 and TRPML3 isoforms, exhibiting EC50 values of 2.7 μM and 10.8 μM, respectively, while serving as a potent inhibitor of TRPML1 with an IC50 of 5.9 μM. This compound facilitates investigations into lysosomal ion channel functions, cellular ion homeostasis, and related signaling pathways. Its unique pharmacological profile makes it a valuable tool for researchers studying the role of TRPML channels in various biological processes. -
TRPM6 Inhibitor
Mesendogen is a selective TRPM6 inhibitor that plays a crucial role in the regulation of magnesium homeostasis. It enhances the differentiation of human embryonic stem cells (hESCs) and human induced pluripotent stem cells (hiPSCs) into mesodermal and definitive endoderm lineages. This compound is valuable for research focused on early embryonic development and the role of magnesium in cellular processes. -
TRP Channel Agonist
Podocarpic acid is a natural compound that serves as a TRP channel agonist, specifically activating the TRPA1 channel. This compound demonstrates significant biological activity in modulating sensory nerve pathways and has potential applications in pain research and neurobiology. Its unique pharmacological profile makes it a valuable tool for investigating TRP channel function and related therapeutic targets. -
TRPM8 Antagonist
Elismetrep (MT-8554) is a selective TRPM8 antagonist that inhibits the activity of the transient receptor potential melastatin 8 channel. It is shown to reduce the frequency of vasomotor symptoms and is valuable for research in pain modulation and sensory perception. Elismetrep offers potential applications in the study of disorders related to thermal sensation and nociception. -
TRPV1 Antagonist
TRPV1 antagonist 3 (Compound 7q) is a highly effective antagonist of the TRPV1 receptor, demonstrating an IC50 of 2.66 nM against capsaicin. This compound exhibits mode-selectivity and is characterized by favorable oral bioavailability (F = 60%) as well as the ability to penetrate the central nervous system. TRPV1 antagonist 3 is valuable for research focused on pain modulation and inflammatory processes. -
TRPC6-Specific Agonist
Hyp9 is a potent agonist specific for the transient receptor potential canonical 6 (TRPC6) channel. This compound facilitates TRPC6 activation, making it a valuable tool for investigating its role in cellular signaling pathways and the pathophysiology of spinal cord injury (SCI). Researchers can utilize Hyp9 to explore therapeutic strategies targeting TRPC6 in models of neuroprotection and regeneration. -
TRPA1 Activator
Supercinnamaldehyde is a potent activator of the transient receptor potential ankyrin 1 (TRPA1) channel, exhibiting an EC50 value of 0.8 μM. It activates TRPA1 through covalent modification of cysteine residues, making it a valuable tool for studying pain pathways and sensory signaling. Its applications include research into inflammation, nociception, and neurobiology. -
TRPV4 Antagonist
PF-05214030 is a potent TRPV4 antagonist, exhibiting IC50 values of 4 nM for human TRPV4 and 27 nM for rat TRPV4. This compound effectively counteracts the decrease in bladder capacity induced by intravesical administration of a TRPV4 agonist. PF-05214030 is therefore a valuable tool for investigating the role of TRPV4 in bladder physiology and may hold potential for therapeutic applications in bladder dysfunction research. -
TRPC4/TRPC5 Channel Inhibitor
ML204 hydrochloride is a selective inhibitor of the TRPC4 and TRPC5 channels, demonstrating a minimum of 19-fold selectivity over the TRPC6 channel. It has no significant effects on other transient receptor potential (TRP) channels or on voltage-gated sodium, potassium, or calcium channels. This compound is valuable for research applications exploring cellular calcium signaling and the physiological roles of TRPC4 and TRPC5 in various biological processes. -
TRPV1 Agonist
MDR-652 is a targeted agonist of the transient receptor potential vanilloid 1 (TRPV1) channel. This compound displays high specificity with binding affinities (Kis) of 11.4 nM for human TRPV1 and 23.8 nM for rat TRPV1. The effective concentrations (EC50s) are 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 demonstrates significant potential as a topical analgesic, making it a valuable tool in pain research and therapeutic applications. -
TRPC5 Inhibitor
GFB-8438 is a highly selective inhibitor of the transient receptor potential channel TRPC5, exhibiting IC50 values of 0.18 μM for hTRPC5 and 0.29 μM for hTRPC4. This compound demonstrates significant selectivity over TRPC6, other TRP family members, NaV 1.5, and shows minimal activity against the hERG channel. GFB-8438 has been shown to provide protective effects to mouse podocytes from injury induced by protamine sulfate, highlighting its potential for research in renal protection and related pathways. -
TRPC5 Antagonist
Evifacotrep is a potent antagonist of the transient receptor potential channel 5 (TRPC5) with an IC50 of ≤50 nM. This compound effectively inhibits TRPC5/TRPC4 activity, making it a valuable tool for investigating neurological diseases. Its selective mechanism of action allows for detailed study of TRPC channel involvement in various pathophysiological processes. -
TRPC3 Inhibitor
JW-65 is a selective inhibitor of the TRPC3 channel, targeting its role in various cellular processes. This compound exhibits significant biological activity that can be leveraged in studies of neurological and cardiovascular diseases. JW-65 is useful for investigating the mechanisms of TRPC3 in pathophysiological conditions and may provide insights into potential therapeutic applications. -
TRPV3 Inhibitor
17(R)-Resolvin D1 is a TRPV3 inhibitor known for its potent anti-inflammatory properties. This aspirin-triggered epimer of Resolvin D1 exhibits significant biological activity by specifically inhibiting TRPV3 with an IC50 of 398 nM. It has demonstrated peripheral anti-nociceptive efficacy, making it a valuable tool for research applications focused on inflammation and pain management. -
TRPC3/C6/C7 Activator
L687 is a potent activator of the TRPC3, TRPC6, and TRPC7 channels, facilitating the cellular uptake of oligonucleotides. Its ability to modulate calcium influx makes it a valuable tool for studying TRP channel function and its role in various physiological processes. L687 has potential applications in molecular biology, particularly in gene delivery and therapeutic research involving nucleic acid-based strategies. -
TRPC6 PAM
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) targeting TRPC6 channels. This compound significantly enhances channel activation at low basal concentrations of diacylglycerol (DAG), facilitating increases in intracellular calcium ([Ca2+]i) levels in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 serves as an essential reagent for researchers investigating TRPC6-dependent signaling pathways and calcium dynamics. -
TRPV1 Agonist
Capsiate is a TRPV1 agonist derived from a non-pungent variety of CH-19 sweet red pepper. This compound exhibits potent biological activity by activating the transient receptor potential vanilloid 1 (TRPV1) channel, which is involved in the modulation of pain and inflammation pathways. Capsiate is utilized in research applications focused on pain management, metabolic studies, and the exploration of sensory receptor functions. -
TRPV4 Receptor Antagonist
RN-9893 is a potent and selective antagonist of the TRPV4 receptor, exhibiting IC50 values of 320 nM, 420 nM, and 660 nM for mouse, human, and rat channels, respectively. This compound is valuable for research applications involving the modulation of TRPV4-mediated physiological processes. Its selective inhibition can aid in studies related to pain sensation, inflammation, and other TRPV4-associated diseases. -
Insecticide
Afidopyropen is an insecticide that targets sucking insects, including whiteflies, aphids, and leafhoppers. It operates by influencing the Nanchung (Nan) and Inactive (Iav) genes in these insects, thereby affecting the TRPV channel. Due to its degradability, Afidopyropen is suitable for use on a variety of crops, making it a valuable tool in agricultural research and pest management. -
TRPA1 Agonist
(E)-4-Oxo-2-nonenal is a potent agonist of the transient receptor potential ankyrin 1 (TRPA1) channel, identified as a significant product of lipid hydroperoxide decomposition. This compound plays a crucial role in mediating oxidative stress responses and has been implicated in various pathological conditions. It is useful in research applications exploring TRPA1-related signaling pathways and the impact of oxidative stress on cellular functions. -
TRPM2 Inhibitor
TAT-M2NX is a selective inhibitor of the human TRPM2 channel, playing a crucial role in modulating calcium influx induced by hydrogen peroxide. This compound demonstrates neuroprotective effects in models of ischemic stroke, preserving hippocampal long-term potentiation and improving memory function following traumatic brain injury. Additionally, TAT-M2NX reduces infarct volume after middle cerebral artery occlusion, although its effects have not been observed in female mice. This reagent is valuable for research applications related to traumatic brain injury and ischemic stroke. -
TRPC5 Inhibitor
TRPC5-IN-1 is a selective TRPC5 inhibitor that demonstrates 50.5% inhibition of TRPC5 at a concentration of 3 μM. This compound is valuable for studying the role of TRPC5 in chronic kidney disease (CKD) and may facilitate research aimed at understanding the underlying mechanisms of renal pathophysiology. Its specificity makes it a useful tool in investigating potential therapeutic interventions targeting TRPC5-related pathways. -
TRP Channel
Cryosim-3 is a selective agonist of the TRPM8 receptor, known for its role in thermosensation and chemosensation. This compound enhances tear secretion and alleviates ocular discomfort in various animal models, making it valuable for research in ocular therapeutics and sensory biology. Its application may extend to understanding the modulation of pain and inflammation through TRP channel pathways. -
TRPV4 Inhibitor
RN-1665 is an orally active TRPV4 inhibitor, demonstrating high selectivity for other related TRP receptors, including TRPV1, TRPV3, and TRPM8. This compound serves as an effective probe for screening TRPV4 interactions, exhibiting IC50 values of 0.26 μM and 0.39 μM for human TRPV4 and rat TRPV4, respectively. RN-1665 is valuable for research applications focused on pain pathways, sensory physiology, and potential therapeutic interventions targeting TRPV4-mediated processes. -
TRPV Activator
N-Arachidonoyl Taurine is a selective activator of the transient receptor potential vanilloid channels TRPV1 and TRPV4, exhibiting EC50 values of 28 μM and 21 μM, respectively. This compound is pivotal in studies investigating pain perception, thermoregulation, and various neurophysiological processes. Its unique properties make it a valuable tool for researching TRPV-mediated signaling pathways and their implications in sensory biology. -
TRPA1 Antagonist
LY3526318 is a selective antagonist of the TRPA1 ion channel, with an IC50 of 5-6 μM. This compound effectively inhibits TRPA1-mediated pain signal transduction, demonstrating notable analgesic activity. LY3526318 is primarily utilized in research focused on chronic pain conditions, including diabetic peripheral neuropathy, chronic low back pain, and osteoarthritis-related pain. -
TRPA1 Inhibitor
TRPA1-IN-2 is a potent inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel, exhibiting an IC50 of 0.04 µM. This compound demonstrates significant anti-inflammatory properties, making it a valuable tool for research into pain pathways and inflammatory diseases. Its oral bioavailability further enhances its utility in preclinical studies aimed at targeting TRPA1-related conditions. -
TRPV1 Antagonist
SB 452533 is a potent and selective antagonist of the TRPV1 ion channel. It demonstrates a pKb of 7.8, indicating strong binding affinity and inhibitory activity. This compound is primarily utilized in research applications related to pain modulation and inflammation, offering insights into the role of TRPV1 in nociception and sensory neurons. SB 452533 is an essential tool for studying pain pathways and developing potential analgesic therapies. -
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.
