TRP Channel

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.

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.

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.

(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.

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.

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.

(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.

MSK-195 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating a potency of 120 nM and an efficacy of 71% in inducing arteriolar responses. This compound is valuable for research applications aimed at understanding pain pathways, neurogenic inflammation, and the physiological role of TRPV1 in various tissues. Its ability to selectively activate TRPV1 makes it a useful tool for dissecting the functions and mechanisms associated with this receptor in preclinical studies.

A778317 is a potent TRPV1 antagonist, designed to inhibit the activation of TRPV1 receptors. With a pIC50 value of 8.31, it effectively blocks intracellular calcium level changes mediated by TRPV1. This compound has demonstrated the capability to prevent capsaicin and acid-induced activation of natural rat TRPV1 receptors in dorsal root ganglion neurons, making it a valuable tool for research focused on pain mechanisms and sensory nerve function.

Cyclo(-asp-gly) is a cyclic dipeptide that functions as a TRPV1 stimulator, enhancing the activity of the transient receptor potential vanilloid 1 ion channel. This compound is utilized in research applications related to pain signaling and sensory perception, making it a valuable tool in studies focused on nociception and the mechanisms of pain modulation. Its role in activating TRPV1 provides insights into potential therapeutic approaches for pain management.

JYL-79 is a potent TRPV1 agonist, exhibiting an IC50 of 3.9 nM. It is primarily used in research focused on neuropathic pain, allowing for the exploration of TRPV1's role in pain pathways and potential therapeutic interventions. This compound provides valuable insights into the mechanisms of pain modulation and serves as a tool for investigating the biology of sensory neurons.

TRPV3 modulator-1 is a selective modulator of the transient receptor potential vanilloid 3 (TRPV3) channel. It exhibits the ability to regulate TRPV3 activity, influencing calcium ion influx in response to thermal and chemical stimuli. This compound has potential applications in research related to pain sensation, skin physiology, and itch, making it a valuable tool for studying TRPV3-mediated signaling pathways.

M084 hydrochloride is a selective inhibitor of the TRPC4 and TRPC5 ion channels, exhibiting IC50 values of 10.3 μM and 8.2 μM, respectively. This compound demonstrates significant antidepressant and anxiolytic effects, making it a valuable tool for studying anxiety and mood disorders. Its ability to modulate calcium influx through TRPC channels positions M084 hydrochloride as an important reagent for research in neurobiology and pharmacology.

TRPV4 antagonist 5 is a selective antagonist of the TRPV4 channel, which is involved in various physiological processes including osmoregulation and pain sensation. This compound demonstrates potential in modulating TRPV4-mediated responses and can be utilized in research focusing on inflammation, pain management, and sensory neuronal pathways. Its application may also extend to investigations of cellular calcium signaling and the development of therapeutics targeting TRPV4-related disorders.

AC4 is a potent TRPV1 antagonist that acts as a trans antagonist upon voltage activation of the receptor and functions as a cis antagonist in response to capsaicin stimulation. This compound serves as a valuable tool for investigating TRPV1 signaling pathways and the modulation of nociceptive responses. Its unique photoswitchable properties allow for the combined use of an antagonist and an agonist, making it an essential reagent for research in pain mechanisms and sensory biology.

AMG-628 is a potent orally active inhibitor of the transient receptor potential vanilloid 1 (TRPV1). It effectively blocks capsaicin and acid-induced calcium influx in TRPV1-expressing CHO cells, with IC50 values of 4.9 nM and 3.1 nM, respectively. AMG-628 demonstrates significant analgesic effects in capsaicin-induced rat pain models and has a half-life of approximately 2.4 hours in rats, making it a valuable tool for studying pain mechanisms and potential therapeutic applications.

TRPC3/6-IN-1 is a selective blocker of the canonical transient receptor potential channels TRPC3 and TRPC6, exhibiting IC50 values of 1260 nM and 500 nM, respectively. This compound is instrumental for investigating the role of TRPC3 and TRPC6 in cardiac physiology and pathophysiology, particularly in chronic models of heart failure. Its specific inhibitory action makes it a valuable tool for studying the mechanisms underlying cardiovascular diseases.

Ibuprofen acyl-β-D-glucuronide is a selective antagonist of the TRPA1 ion channel. This compound effectively reduces the calcium response induced by allyl isothiocyanate (AITC), exhibiting an IC50 value of 60 μM. It is a valuable tool for investigating TRPA1-related pathways and for exploring potential therapeutic applications in pain modulation and sensory signal transduction.

TRPA1-IN-3 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel. This compound is primarily utilized in research focused on skin and respiratory tract conditions, where TRPA1 activation is implicated in nociceptive signaling and inflammatory responses. Its inhibitory properties make it valuable for studying pain mechanisms and potential therapeutic interventions in related disorders.

JNJ-39729209 is a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel, displaying pIC50 values of 7.9 to 8.5 across various species including human, rat, canine, and guinea pig. This compound effectively inhibits capsaicin-induced hypotension and associated hypothermia. Additionally, JNJ-39729209 demonstrates significant anti-inflammatory and analgesic effects in carrageenan and CFA-induced thermal hyperalgesia models in rats, as well as anti-cough activity in guinea pigs, making it a valuable tool for research in pain and inflammatory response.

TRPV Antagonist 1 is a selective transient receptor potential vanilloid (TRPV) channel antagonist, exhibiting an IC50 of less than 250 nM. This compound effectively inhibits TRPV-mediated calcium influx, making it a valuable tool for investigating TRPV-related signaling pathways. It is applicable in research focused on pain, inflammation, and sensory neuron function, facilitating the study of TRPV channels in various biological contexts.

Farnesyl pyrophosphate-d6 is a deuterium-labeled stable isotope derivative of farnesyl pyrophosphate, an important metabolic intermediate in the mevalonate pathway. It acts as an agonist for TRP channel TRPM2, facilitating calcium influx and promoting cell death. Farnesyl pyrophosphate plays a crucial role in cholesterol and ubiquinone synthesis, as well as in protein farnesylation and geranylgeranyl pyrophosphate synthesis. This reagent is utilized in research exploring cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders.

Linopirdine is a selective inhibitor of the M-type potassium current (IM; Kv7; KCNQ channels) with an IC50 of 2.4 μM. This compound exhibits potential as a cognition-enhancing agent by promoting acetylcholine release in rat brain tissue. Linopirdine is primarily utilized in research focused on understanding cognitive function and the modulation of neurotransmitter release. Additionally, its role as a TRPV1 agonist provides further avenues for investigation in neurobiology and pharmacology.

JNc-440 is a TRPV4-KCa2.3 interaction enhancer with significant potential as an antihypertensive agent. This compound promotes the interaction between the transient receptor potential vanilloid 4 (TRPV4) and the calcium-activated potassium channel 3 (KCa2.3) in endothelial cells, resulting in enhanced vasodilation. Furthermore, JNc-440 demonstrates effective antihypertensive properties in murine models, making it a valuable tool for cardiovascular research.

NS8593 is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels), specifically targeting the SK1-3 subtypes. It exhibits a reversible inhibition of SK3-mediated currents with Ca2+-dependent potency (Kd values of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), while leaving intermediate and large conductance K channels unaffected. Additionally, NS8593 inhibits the TRPM7 channel with an IC50 of 1.6 mM. This compound is valuable for research into central nervous system-related diseases and the physiological roles of SK and TRPM7 channels.

ErSO-TFPy is a selective activator of the TRPM4 ion channel, designed for studying its effects on calcium and sodium ion homeostasis in cells. This compound exhibits low nanomolar cytotoxicity specifically towards ERα+ breast cancer cells, leading to dysregulation of calcium balance and triggering an anticipatory unfolded protein response. The resultant cellular stress induces immune cell-independent necrotic cell death. ErSO-TFPy is a valuable tool for investigating the mechanisms underlying estrogen receptor alpha positive breast cancer.

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.

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.

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.

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.

CAY10448 is a 6-Iodonordihydrocapsaicin analogue that selectively modulates the transient receptor potential vanilloid 1 (TRPV1) channel. This compound serves as a valuable tool for research into pain pathways and sensory neuron activation. Its ability to interact with TRPV1 makes it useful for studies investigating pain mechanisms, neuroprotective effects, and the modulation of inflammatory responses.

08:0 PI(4,5)P2 ammonium is a biochemical assay reagent that targets lipid signaling pathways. Its primary application involves probing the binding site at the transient receptor potential vanilloid 4 (TRPV4) N-terminus. This compound facilitates the study of cellular mechanisms influenced by phosphoinositides, contributing valuable insights into TRPV4-related functions in various physiological contexts.

16-HydroxyCapsaicin is a natural product derived from chili peppers, exhibiting its biological activity primarily through interaction with TRPV1 (transient receptor potential vanilloid 1) channels. This compound is known for its potential analgesic and anti-inflammatory properties, making it a valuable reagent for research in pain relief and sensory biology. Its unique mechanism of action underscores its relevance in studies exploring the modulation of pain pathways and the physiological responses to capsaicinoids.

17-Hydroxy Capsaicin is a natural product derived from chili peppers, exhibiting significant activity as a vanilloid receptor (TRPV1) agonist. This compound is known to modulate pain perception and has demonstrated anti-inflammatory properties. Its applications in research include exploring mechanisms of pain relief and the development of novel analgesics, making it a valuable tool in pharmacological studies.

5-Amino-2-methoxyphenol is a phenolic regioisomer that exhibits significant antinociceptive properties. In the mouse formalin test, it demonstrates dose-dependent analgesic effects, with its second-phase action involving both fatty acid amide hydrolase (FAAH) and transient receptor potential vanilloid 1 (TRPV1). This compound is valuable for research focused on pain mechanisms and potential therapeutic applications in pain management.

Ovalicin is a selective inhibitor of the transient receptor potential vanilloid 1 (TRPV1), exhibiting significant anti-inflammatory and anti-atopic dermatitis effects. It covalently binds to MetAP2, inhibiting its activity and demonstrating efficacy against pathogens such as Enterocytozoon bieneusi. Through the attenuation of LPS-induced calcium influx and modulation of inflammatory gene expression, Ovalicin effectively reduces macrophage and mast cell infiltration in the skin, alleviating allergic symptoms in mouse models. This compound is valuable for research into microsporidiosis and atopic dermatitis.