TRP Channel

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.

TRPV1 Antagonist 11 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 29.3 nM. Additionally, it serves as a μ-opioid receptor (MOR) agonist with a Ki value of 60.3 nM. This compound demonstrates significant analgesic properties by antagonizing TRPV1, thereby reducing pain signaling, and activating MOR, which enhances the pain-relief effect. TRPV1 Antagonist 11 has been shown to provide a robust, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice, making it a valuable tool for pain research.

Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas.

(Thr4,Gly7)-Oxytocin is a specific agonist of the oxytocin receptor (OT receptor). This analogue enhances neuronal excitability in subicular neurons through the activation of TRPV1 channels and the inhibition of K+ channels. Its unique properties make it valuable for research applications involving neurobiology and the study of oxytocin-related pathways.

(±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels.

N-Oleoyl Taurine is an endogenous metabolite that acts as an amino-acyl endocannabinoid. It is known to activate transient receptor potential (TRP) channels, specifically TRPV1 and TRPV4, implicating its role in calcium signaling. This compound has been isolated from rat brain and presents potential applications in research studying the physiological effects of TRP channel modulation and its involvement in neurological functions.

N-Lignoceroyl Taurine is an endogenous metabolite and taurine conjugate of lignoceric acid, identified through lipidomic analysis of bovine brain. This compound exhibits distinct biological activity as a substrate for fatty acid amide hydrolase (FAAH), with levels significantly elevated in FAAH knockout mice, indicating a potential role in lipid metabolism. Additionally, N-Lignoceroyl Taurine has been shown to activate transient receptor potential (TRP) calcium channels, including TRPV1 and TRPV4, highlighting its relevance in neurobiology and cellular signaling research.

Stearoyl serotonin is a hybrid compound designed to target the endogenous metabolite systems and is structurally derived from arachidonoyl serotonin. This compound is investigated for its ability to function as a dual antagonist of fatty acid amide hydrolase (FAAH) and the TRPV1 channel, which are critical pathways in the modulation of pain. Preliminary studies suggest that modifications to the arachidonoyl structure, such as the introduction of an 18-carbon stearoyl moiety, may influence TRPV1 channel activity; replacement with saturated fatty acids has demonstrated significant inhibition of capsaicin-induced activation. This positions stearoyl serotonin as a potential candidate for research into pain mechanisms and therapeutic applications.

SU200 is a TRPV1 agonist that modulates intracellular calcium ion concentrations. It induces distinct calcium ion response patterns, displaying notable reactivity and peak efficacy. The effects of SU200 exhibit varying degrees of response delay and variability across different cell types. This compound offers potential avenues for pharmacological development and further research into calcium signaling pathways.

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.

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.

KM-001-E2 is the (S)-enantiomer of KM-001, a selective antagonist of the TRPV3 channel. This compound plays a significant role in investigating the mechanisms underlying skin itching and keratinization disorders. Its application in research may provide insights into TRPV3-related pathophysiology and potential therapeutic strategies for skin conditions.

Camphor ((±)-Camphor) is recognized as a TRP channel agonist, primarily targeting TRPV3. This compound exhibits notable antiviral, antitussive, and anticancer activities, making it valuable for various research applications. Although utilized topically for its anti-infective and anti-pruritic properties, caution is advised as camphor can be toxic when ingested. Its diverse biological activities make it a significant candidate for studies related to TRPV channel modulation.

Vanillyl butyl ether serves as a repellent agent primarily through its modulation of TRPV1 and TRPM8 channels in mammalian systems. This compound exhibits notable activity against pests such as Tribolium castaneum, T. confusum, and L. bostrychophila, demonstrating its potential in pest control applications. Additionally, it acts as a mild warming agent, promoting enhanced blood circulation while retaining its eco-friendly and non-toxic profile.

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.

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.