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Transient receptor potential (TRP) channel modulators act on cation channels that sense heat, cold and irritants. The mammalian family has six subfamilies, including vanilloid (TRPV), ankyrin (TRPA), canonical (TRPC) and melastatin (TRPM) channels. TRP channels respond to temperature, touch, osmotic changes and plant-derived compounds, so they are often described as cellular sensors. Cloning of the capsaicin receptor TRPV1 in 1997 identified it as a heat-activated ion channel in pain-sensing neurons. AMG517 and SB-705498 are TRPV1 antagonists, while A 967079 blocks TRPA1 and optovin activates TRPA1 when exposed to light. Pyr10 inhibits TRPC3, and Pico145 inhibits channels formed by TRPC1, TRPC4 and TRPC5. The spider toxin peptide GsMTx4, an inhibitor of mechanosensitive channels, is also listed under Piezo 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.
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.
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.
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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.
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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.
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-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.
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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-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.
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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-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.
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.
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-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.
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.
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.
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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.
Synonyms: MK-056
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.
Synonyms: NGD-8243
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.
Synonyms: 8-Bromoadenosine-5'-O-diphosphoribose
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.
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.
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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.
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-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.
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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.
