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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
TRPV4 Inhibitor
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. -
TRP Channel Inhibitor
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 Inhibitor
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. -
FAAH Inhibitor and TRPV1 Antagonist
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. -
TRPM3 Inhibitor
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. -
TRPM7 Inhibitor
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 Inhibitor
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. -
TRP Channel Inhibitor
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 Inhibitor
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 Inhibitor
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 Inhibitor
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. -
ACU Inhibitor/VR1 Agonist
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 Inhibitor
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. -
TRPM7 Inhibitor
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. -
TRPM2 Inhibitor
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. -
TRPM2 Channel Inhibitor
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 Inhibitor
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. -
TRPA1 Inhibitor
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 Inhibitor
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 Inhibitor
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. -
TRPV2 Channel Inhibitor
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 Inhibitor
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. -
TRP Channel Inhibitor
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. -
TRPC4/5 Inhibitor
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. -
TRPV1 Inhibitor
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 Inhibitor
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. -
URAT Inhibitor
Xininurad is a selective urate transporter (URAT) inhibitor that modulates uric acid levels in the body. By inhibiting URAT, it promotes renal excretion of uric acid, making it a valuable tool for studying hyperuricemia and related conditions such as gout. This compound serves as a potential therapeutic agent in research aimed at understanding and treating disorders associated with elevated urate concentrations. -
URAT1 Inhibitor
URAT1 inhibitor 3 is a selective inhibitor of the urate transporter 1 (URAT1), demonstrating a potent inhibition with an IC50 value of 0.8 nM. This compound effectively lowers urate levels, making it valuable for studies focused on gout and hyperuricemia. Its oral bioavailability allows for convenient administration in various biological assays and preclinical research settings. -
URAT1 Inhibitor
Ruzinurad is a highly selective inhibitor of the URAT1 transporter, which plays a critical role in the regulation of uric acid levels. By inhibiting URAT1, Ruzinurad effectively reduces uric acid reabsorption, making it a valuable tool in the study of hyperuricemia and related metabolic disorders. This compound has potential applications in research focusing on conditions such as gout and other diseases associated with elevated uric acid levels. -
URAT Inhibitor
Puliginurad is a potent inhibitor of the urate transporter (URAT), which plays a critical role in uric acid reabsorption in the renal system. This compound is valuable for research in hyperuricemia and gout, offering insights into uric acid metabolism and potential therapeutic interventions. Its application in experimental studies can help elucidate the mechanisms underlying these conditions and support the development of novel treatment strategies. -
URAT1 Inhibitor
URAT1 inhibitor 6 is a selective inhibitor of the urate transporter URAT1, exhibiting an IC50 value of 35 nM for human URAT1. This compound demonstrates significantly enhanced potency compared to its parent compound, Lesinurad, and the reference compound Benzbromarone. URAT1 inhibitor 6 is valuable for investigating uric acid transport and inflammation-related research applications. -
URAT1 Inhibitor
URAT1 inhibitor 8 is a potent inhibitor of the urate transporter URAT1, exhibiting an IC50 of 0.001 μM. This compound is valuable for research applications focused on gout, offering insights into mechanisms of uric acid regulation and potential therapeutic strategies for hyperuricemia. Its high efficacy makes it a significant tool for studying renal handling of urate and related disorders. -
Xanthine Oxidase Inhibitor
URAT1&XO Inhibitor 1 is a dual inhibitor targeting both URAT1 and Xanthine Oxidase, with IC50 values of approximately 10 μM and 1.01 μM, respectively. This compound effectively induces a hypouricemic effect in a potassium oxonate-induced hyperuricemia rat model. URAT1&XO Inhibitor 1 is valuable for research applications focused on hyperuricemia and related disorders. -
URAT1&XO Inhibitor
URAT1&XO Inhibitor 2 is a dual inhibitor targeting xanthine oxidase and URAT1, exhibiting an IC50 of 3.3 μM for xanthine oxidase. This compound effectively inhibits uric acid uptake in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. In hyperuricemic mouse models, it has been shown to reduce serum urate levels and decrease uric acid excretion. URAT1&XO Inhibitor 2 is valuable for researching conditions related to hyperuricemia. -
hURAT1 Inhibitor
hURAT1 inhibitor 2 is a selective inhibitor of hURAT1 (uric acid transporter 1, SLC22A12), exhibiting an IC50 of 18 nM. Additionally, it demonstrates moderate inhibitory activity on OATP1B1 with an IC50 of 0.73 μM. This compound is valuable for research focused on disorders associated with dysregulated uric acid metabolism, including hyperuricemia and gout. -
URAT1 Inhibitor
Lingdolinurad is a selective inhibitor of the urate transporter URAT1. It effectively reduces urate reabsorption, making it a valuable tool in studying hyperuricemia. This compound can be applied in both in vitro and in vivo research to explore its potential therapeutic effects and underlying mechanisms in disorders associated with elevated uric acid levels. -
URAT1 Inhibitor
JTT-552 is a selective URAT1 inhibitor known for its ability to reduce uric acid reabsorption in the renal system. This compound demonstrates significant potential in managing hyperuricemia and treating gout by promoting uric acid excretion. Its application in research can aid in understanding the pathophysiology of gout and developing therapeutics aimed at uric acid regulation.
