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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
URAT1 Inhibitor
URAT1 inhibitor 7 is a potent inhibitor of the urate transporter URAT1, demonstrating an IC50 of 12 nM. This compound exhibits excellent microsomal stability, with a hepatic microsomal clearance rate of less than 13 µL/min/mg. Additionally, it has been shown to inhibit CYP2C9 with an IC50 of 4.2 µM. URAT1 inhibitor 7 is suitable for research applications focused on gout and related disorders. -
XOR/URAT1 Inhibitor
XOR/URAT1-IN-1 is a dual inhibitor targeting xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), exhibiting IC50 values of 6 nM and 12.9 μM, respectively. This compound effectively reduces uric acid levels in models of acute hyperuricemia induced by potassium oxonate or hypoxanthine. It serves as a valuable tool for studying disorders related to hyperuricemia and offers potential therapeutic insights for conditions such as gout. -
URAT1 Inhibitor
URAT1 Inhibitor 10 is a potent inhibitor of the URAT1 transporter, demonstrating high selectivity for OAT1. This compound exhibits oral bioavailability and low cytotoxicity, making it suitable for in vivo studies. It is primarily used in research applications focused on renal physiology and uric acid transport, aiding investigations into gout and related disorders. -
URAT1 Inhibitor
Darbinuradum is an inhibitor of the urate transporter URAT1, primarily impacting uric acid reabsorption in the renal proximal tubule. This compound demonstrates significant potential in research related to hyperuricemia and gout management by reducing uric acid levels in plasma. It is utilized in studies investigating the therapeutic effects of urate-lowering therapies and their implications for cardiovascular health and kidney function. -
URAT1 Inhibitor
URAT1 inhibitor 13 is a selective inhibitor of the urate transporter 1 (URAT1), which is primarily involved in renal urate reabsorption. This compound exhibits strong biological activity in reducing urate levels and is particularly relevant in the study of gout and other related hyperuricemia conditions. Researchers can utilize URAT1 inhibitor 13 to explore its therapeutic potential and the underlying mechanisms in urate regulation. -
URAT1 Inhibitor
URAT1 inhibitor 2 is a potent inhibitor of the URAT1 transporter, exhibiting an IC50 of 1.36 µM for URAT1-mediated 14C-UA uptake, alongside effective inhibition of CYP1A2 and CYP2C9 with IC50 values of 16.97 µM and 5.22 µM, respectively. This compound demonstrates significant potential in the investigation of hyperuricemia and gout, making it a valuable tool for biochemical research and therapeutic development. -
URAT1 Inhibitor
URAT1 Inhibitor 5 is an effective inhibitor of the urate transporter URAT1. This compound has demonstrated potential in modulating uric acid reabsorption, making it relevant for the investigation of hyperuricemia and related conditions. Its application in biochemical research can facilitate the development of therapeutics targeting disorders associated with elevated uric acid levels. -
URAT1 Inhibitor
URAT1 Inhibitor 9 targets the urate transporter URAT1, playing a crucial role in regulating uric acid levels. This compound demonstrates significant biological activity in the management of gout and hyperuricemia by inhibiting uric acid reabsorption in the kidneys. URAT1 Inhibitor 9 is valuable for research focusing on urate homeostasis and associated metabolic disorders. -
URAT1 Inhibitor
URAT1 Inhibitor 11 is a potent inhibitor of the URAT1 transporter, exhibiting an IC50 value of 0.18 μM. This compound demonstrates significant hypouricemic effects in hyperuricemic zebrafish models induced by potassium oxonate and xanthine sodium salt. URAT1 Inhibitor 11 serves as a valuable tool for research applications focused on hyperuricemia and related metabolic disorders. -
URAT1/XO Inhibitor
URAT1&XO Inhibitor 3 is a potent inhibitor of both xanthine oxidase (XO) and urate transporter 1 (URAT1), with IC50 values of 35 nM and 31 nM, respectively. This compound exhibits significant potential as an orally active anti-gout agent, demonstrating favorable pharmacological and pharmacokinetic properties. Additionally, URAT1&XO Inhibitor 3 has been shown to have in vivo safety, making it a valuable tool for research in the management of hyperuricemia and gout-related disorders. -
URAT1 Inhibitor
HC-1310 is a potent inhibitor of URAT1, a transporter involved in uric acid reabsorption in the renal system. This compound is primarily utilized in research focused on hyperuricemia and gout, providing valuable insights into therapeutic strategies for managing elevated uric acid levels. By inhibiting URAT1, HC-1310 facilitates increased uric acid excretion, making it a critical tool for studying conditions associated with abnormal purine metabolism. -
URAT1 Inhibitor
URAT1-IN-14 is a potent inhibitor of the urate transporter 1 (URAT1), demonstrating a human URAT1 inhibition IC50 of 0.72 μM in HEK293 cells. This compound exhibits minimal cytotoxicity in Hep-G2 cells, making it suitable for cellular applications. URAT1-IN-14 has been shown to effectively reduce urate levels in hyperuricemia mouse models, supporting its use in research related to hyperuricemia and gout. -
Calcium Channel Inhibitor
ω-Hexatoxin-Hv1a is a selective inhibitor of L-type voltage-dependent calcium channels. This neurotoxin reduces intracellular calcium ion concentration, thereby mitigating apoptosis, necroptosis, and oxidative stress, while enhancing cellular recovery and energy levels. Its ability to induce paralysis and mortality in insects through the disruption of central nervous system neurotransmission underscores its potency, although it has limited oral toxicity. Consequently, ω-Hexatoxin-Hv1a is a valuable tool for research into ischemia-reperfusion injury, atopic dermatitis, and ischemic damage in cardiomyocytes and neurons. -
T-Type Calcium Channel Inhibitor
T-Type Calcium Channel Inhibitor 2 is a selective inhibitor of T-type calcium channels, specifically targeting Cav3.1 (α1G), Cav3.2 (α1H), and Cav3.3 (α1I), with IC50 values of 31.0, 83.1, and 69.3 µM, respectively. This compound exhibits significant cytotoxic activity against A549 and HCT-116 cancer cell lines, with IC50 values of 5.0 and 6.4 µM. It serves as a useful tool in the investigation of calcium channel involvement in various physiological processes and potential therapeutic targets in cancer research. -
Ca2+‑ATPase Inhibitor
rel-(E)-6,7-Transdihydroxyligustilide is a potent inhibitor of Ca2+-ATPase, specifically in calmodulin-deficient human erythrocyte membranes. This compound, derived from the dried tuberous roots of Polygonum multiflorum, plays a significant role in the regulation of calcium homeostasis. It is particularly valuable in research related to hyperlipidemia and related metabolic disorders. -
SERCA Inhibitor
4,4'-Methylenebis(2,6-di-tert-butylphenol) is a selective inhibitor of sarco/endoplasmic reticulum calcium ATPase (SERCA), with an IC50 value of 17 μM. This compound plays a critical role in modulating calcium homeostasis and is valuable for research into cellular processes and disorders linked to calcium dysregulation. Its application extends to studying various diseases where altered calcium signaling is implicated. -
Calcium Channel Inhibitor
A-39355 is a calcium channel inhibitor that effectively reverses multidrug resistance in tumor cells. It enhances the cytotoxicity of antitumor compounds by increasing their accumulation within resistant cells and inhibiting their efflux. Unlike traditional calcium antagonists, A-39355 exhibits minimal hypotensive effects. This compound is particularly useful for research focused on overcoming treatment resistance in cancer therapy. -
L-type Calcium Channel Inhibitor
Diltiazem malate is a potent inhibitor of L-type calcium channels, effectively modulating calcium influx in cardiac and vascular smooth muscle. It exhibits significant antihypertensive and antiarrhythmic properties, making it valuable for the investigation of cardiovascular conditions. Diltiazem malate is commonly used in research related to cardiac arrhythmia, hypertension, and angina pectoris.
