TRP Channel

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.

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.

TRPV4-IN-5 is a selective TRPV4 inhibitor with an IC50 value of 0.46 μM. This compound exhibits significant efficacy in reducing acute lung injury symptoms induced by lipopolysaccharide in murine models. TRPV4-IN-5 is valuable for research into the modulation of TRPV4-associated pathways and potential therapeutic applications in lung inflammatory conditions.

Cannabidiorcol (CBDO) is an inhibitor of transient receptor potential (TRP) channels. This compound, structurally related to cannabidiol with a shortened pentyl side chain, exhibits anti-inflammatory properties while displaying low affinity for cannabinoid receptors. Research applications include investigations into its potential role in modulating inflammation and exploring its effects on tumorigenesis at elevated concentrations.

TRPV6-IN-1 is a potent and selective inhibitor of the transient receptor potential cation channel subfamily V member 6 (TRPV6). It exhibits significant anti-proliferative effects, making it a valuable tool for cancer research. This compound can be utilized in studies investigating the role of TRPV6 in tumor growth and progression, aiding in the development of potential therapeutic strategies.

N-Arachidonoylserotonin is a potent fatty acid amide hydrolase (FAAH) inhibitor, exhibiting an IC50 value ranging from 1 to 12 µM. Additionally, it serves as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels, with an IC50 of 70 to 100 nM. Due to its dual action, N-Arachidonoylserotonin demonstrates significant analgesic properties in rodent models, making it a valuable tool for research in pain mechanisms and therapeutic interventions.

Ponometrep is a potent antagonist of the transient receptor potential melastatin 3 (TRPM3) channel, exhibiting IC50 values in the range of 1-10 nM. This compound demonstrates significant analgesic activity, making it a valuable tool for the study of pain mechanisms and neurological disorders. Its specificity for TRPM3 allows researchers to explore potential therapeutic applications in related biological pathways.

AAL-149 is a selective inhibitor of the TRPM7 ion channel, exhibiting an IC50 value of 1.081 μM. This compound demonstrates multimodal anti-inflammatory effects while avoiding interaction with sphingosine-1-phosphate (S1P) receptors. AAL-149 is a valuable tool for researchers investigating the role of TRPM7 in inflammation and related biological pathways.

TRPM2-IN-1 is a selective inhibitor of the TRPM2 ion channel, which plays a critical role in calcium influx and cellular signaling. This compound has demonstrated significant neuroprotective effects and exhibits antistroke activity, making it a valuable tool in the study of ischemic stroke and related neurological disorders. Its capacity to modulate TRPM2 activity provides insight into potential therapeutic strategies for neurodegenerative conditions.

HZS60 is a selective TRP channel inhibitor that demonstrates significant neuroprotective effects against cerebral ischemia. It effectively mitigates primary neuronal damage induced by NMDA and oxygen-glucose deprivation/reoxygenation. Additionally, HZS60 exhibits favorable pharmacokinetic properties and can reduce injury associated with cerebral ischemia-reperfusion. This compound serves as a promising candidate for research applications targeting ischemic stroke.

TRPV1-IN-3 is a selective inhibitor of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating significant antifibrotic activity in vitro with an IC50 of 0.51 μM. Its mechanism involves the modulation of fibrosis markers such as collagen I and α-SMA through inhibition of the TGF-β/Smads and MAPK signaling pathways. Research applications include studying idiopathic pulmonary fibrosis, where TRPV1-IN-3 has been shown to reduce collagen deposition in lung tissue, enhance alveolar structure, and increase survival rates in Bleomycin-induced pulmonary fibrosis models.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

(±)-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.

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.

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.

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.