Catalog No.
Product Name
Application
Product Information
Citations
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TRPC3 inhibitor
Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(6):932-940 PMID: 40582844
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TRPV4 ion channel blocker
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. -
TRPV1 receptor antagonist
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM. -
TRPP3 channel inhibitor
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis. -
TRPM8 antagonist
M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively). -
TRPV1 antagonist and TNF-alpha production inhibitor
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor. - Artepillin C is an orally active compound that functions as a CREB/CRTC2 inhibitor and a covalent TRPA1 agonist (EC50 = 1.8 μM). It suppresses CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression, thereby modulating glucose and lipid metabolism. Additionally, Artepillin C activates TRPA1 channels, eliciting spicy taste signals. It exhibits antitumor activity by inhibiting cell proliferation and inducing necroptosis, improves insulin resistance, and reduces hepatic lipid synthesis. Artepillin C is applicable for research into metabolic syndrome, tumor prevention and treatment, and inflammation.
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NMDAR/TRPM4 inhibitor
Brophenexin (compound 8) is a potent inhibitor of the interaction interface between NMDA receptors (NMDAR) and TRPM4 channels, exhibiting significant neuroprotective activity. It prevents NMDA-induced excitotoxicity, including cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. In vivo, Brophenexin protects against brain damage in mice subjected to middle cerebral artery occlusion (MCAO) and preserves retinal ganglion cells from NMDA-induced degeneration. These findings support its potential as a therapeutic agent for neurodegenerative diseases and ischemic brain injury. -
Bacterial Inhibitor
Probenecid is a selective inhibitor of bacterial growth, primarily targeting pannexin 1 channels, while also exhibiting activity as a TRPV2 channel agonist. Its ability to modulate ion channel activity makes it valuable for research into pain pathways and inflammatory responses. Probenecid is commonly used in studies investigating the role of TRPV2 in nociception and as a tool in exploring bacterial resistance mechanisms. -
SOCE/TRPC Blocker
SKF-96365 is a potent blocker of store-operated calcium entry (SOCE) and transient receptor potential (TRPC) channels. By inhibiting these pathways, SKF-96365 effectively reduces intracellular calcium levels, which can lead to calcium overload and cytotoxic effects in glioblastoma cells. Additionally, SKF-96365 disrupts the CaMKIIγ/AKT signaling pathway, inducing apoptosis while promoting protective autophagy in colorectal cancer cells. This compound is valuable for investigating calcium signaling mechanisms and evaluating therapeutic strategies in cancer research. -
TRPC6 Inhibitor
Larixyl acetate is a potent and selective inhibitor of the TRPC6 channel, exhibiting IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. This compound demonstrates significant biological activity by preventing human papillomavirus (HPV) infections and offers protective effects against systemic endothelial dysfunction induced by traumatic brain injury. Larixyl acetate is a valuable tool for research in cellular signaling and the therapeutic exploration of TRPC6-related pathologies. -
TRPM7 Inhibitor
TRPM7-IN-1 is a selective inhibitor of the TRPM7 ion channel, a critical regulator of cellular functions. This compound induces cell cycle arrest and apoptosis in cancer cell lines, such as MCF-7 and BGC-823, while also reducing cell migration. TRPM7-IN-1 modulates expression levels of key proteins, decreasing vimentin and increasing E-cadherin, and acts through the PI3K/Akt signaling pathway. Its ability to diminish TRPM7 expression and function positions TRPM7-IN-1 as a promising candidate for investigation in the context of breast and gastric cancer metastasis. -
TRPV1 Antagonist
TRPV1 Antagonist 10 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 33.06 nM. This compound also demonstrates moderate inhibition of URAT1 (IC50 = 22.51 μM) and partial inhibition of GLUT9 (60.25% at 50 μM). TRPV1 Antagonist 10 is valuable in research applications focusing on analgesia and the management of hyperuricemia, making it a significant tool for studying inflammatory pain mechanisms. -
CB2R Agonist/TRPM8 Antagonist
TRPM8 antagonist 4 acts as a partial agonist of the CB2 receptor (EC50=54.2 nM, Ki=3.2 μM) and an antagonist of the TRPM8 channel (IC50=42.3 nM), demonstrating high functional selectivity. This compound exhibits notable anti-inflammatory and analgesic properties, significantly reducing mRNA expression levels of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β. TRPM8 antagonist 4 is suitable for research applications focused on pain management and inflammation modulation. -
TRPV1 Antagonist
Pellitorine is a natural amide compound that functions as a TRPV1 antagonist, effectively inhibiting pain signal transmission activated by capsaicin. This compound demonstrates significant biological activity by improving cognitive function through the upregulation of BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. In addition, Pellitorine exhibits anti-inflammatory properties by reducing the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Furthermore, it has antithrombotic effects, mitigates lipid peroxidation, and has exhibited activity against Aedes aegypti mosquito larvae as well as certain cancer types and bacteria, making it a versatile tool in chemical research applications. -
hTRPA1 Antagonist
(E)-Cardamonin is a selective antagonist of the human transient receptor potential ankyrin 1 (hTRPA1) channel, exhibiting an IC50 of 454 nM. This compound is instrumental in research involving nociception and inflammatory pain models, facilitating studies of sensory signaling pathways. Its role in modulating hTRPA1 activity makes it a valuable reagent for exploring channel-related physiological and pathological processes. -
Antinociceptive Agent
Citronellyl acetate is a monoterpene compound that serves as an orally active antinociceptive agent. It modulates various targets including TRPV1, TRPM8, ASIC, and glutamate receptors, along with protein kinase pathways PKC and PKA, contributing to its effects on nociception. This compound is valuable for research focused on understanding and managing acute pain mechanisms. -
Stable Isotope
Anandamide-d8 is a deuterated form of the endocannabinoid Anandamide, primarily known for its interaction with cannabinoid receptors CB1 and CB2. This compound modulates various neuronal and immune functions and can also engage additional receptors, including PPARs, TRPV1, and GPR18/GPR55. Anandamide-d8 exhibits potential anti-fungal and anti-inflammatory properties, making it valuable for research applications in fields such as neurodegenerative diseases, including Alzheimer's disease, and inflammatory conditions like ulcerative colitis. -
Stable Isotope
Capsaicin-d3 is a deuterated form of Capsaicin, a well-known TRPV1 agonist derived from chili peppers. This stable isotope allows for precise tracking and analysis in various research applications. Capsaicin-d3 has been implicated in studies exploring analgesic effects for neurological disorders, as well as its potential antioxidant, anti-inflammatory, and anti-cancer properties. Its use in research facilitates a better understanding of pain pathways and the therapeutic potential of capsaicin-related compounds. -
Histamine H1 Receptor/TRPV1 Inhibitor
Dexbrompheniramine is a dual inhibitor of the histamine H1 receptor and the TRPV1 receptor, enabling it to effectively cross the blood-brain barrier. It functions by blocking H1 receptor activity and inhibiting TRPV1-mediated calcium responses in a dose-dependent manner, including responses triggered by Capsaicin. Research indicates that Dexbrompheniramine, when combined with Cimetidine, can mitigate drinking behavior induced by histamine and sham feeding, while it alone does not induce thirst. This compound is valuable for investigating the pathophysiology of chronic cough and related disorders. -
TRPV1 Antagonist
DWP-05195 is a TRPV1 antagonist that inhibits pain signal transduction, providing research applications in pain management studies. Additionally, DWP-05195 induces endoplasmic reticulum (ER) stress-dependent apoptosis in human ovarian cancer cells, mediated by the ROS-p38-CHOP signaling pathway. This compound may be useful for investigating both nociceptive mechanisms and potential therapeutic strategies for ovarian cancer. -
NAAA Inhibitor
AM9053 is a selective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) with an IC50 of 30 nM. It shows limited impact on FAAH activity (IC50 > 100 nM). AM9053 demonstrates significant anti-proliferative effects on colorectal cancer cells through the activation of PPAR-α and TRPV1-dependent pathways, leading to S-phase cell cycle arrest. Additionally, it alleviates intestinal fibrosis by modulating macrophage activity and inhibiting the IL-23 signaling pathway, resulting in increased levels of N-acylethanolamines, particularly palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). AM9053 is valuable for research into colorectal cancer and intestinal fibrosis. -
Inflammation Inhibitor
Resolvin D5 is an anti-inflammatory agent primarily targeting the GPR32 receptor, effectively modulating inflammation responses. It alleviates Paclitaxel-induced mechanical allodynia and inflammatory pain in male mice through mechanisms that do not involve TRPV1 or TRPA1 channels. Resolvin D5 reduces LPS-induced ERK phosphorylation and NF-κB nuclear translocation while downregulating pro-inflammatory mediators, inhibiting Th17 differentiation, and promoting regulatory T cell differentiation. This compound is particularly relevant for research on chemotherapy-induced peripheral neuropathy, inflammatory pain, and rheumatoid arthritis. -
NF-κB Inhibitor/TRP Modulator
Cannabitwinol is a selective NF-κB inhibitor and thermosensitive TRP modulator. It effectively inhibits TNFα-induced NF-κB-driven transcription and IL-8 release, exhibiting notable anti-inflammatory and antioxidant properties. Cannabitwinol selectively activates cold-activated TRP channels, such as TRPA1 (EC50 = 3.0 μM), while antagonizing TRPM8 (IC50 = 3.9 μM), with minimal interaction with heat-activated TRP channels like TRPV1 and TRPV2. This compound is applicable in research focused on inflammatory skin diseases, cold allodynia, and hyperalgesia. -
TRPA1 Agonist
Methyl syringate is a selective agonist of the TRPA1 receptor, playing a crucial role in the regulation of food intake and gastric emptying through TRPA1-mediated pathways. Additionally, this compound functions as an effective phenolic mediator for bacterial and fungal laccases, enhancing their catalytic activities. Methyl syringate serves as a chemical marker in Asphodel monofloral honey and is associated with its antibacterial properties. Furthermore, it has been shown to inhibit aflatoxin production and may contribute to weight suppression, as well as being applicable in research focused on cancer prevention, hypoxia-induced inflammatory response, and tumorigenesis. -
NMDAR/TRPM4 Inhibitor
Brophenexin free base is a potent inhibitor targeting the N-methyl-D-aspartate receptor (NMDAR) and the transient receptor potential melastatin 4 (TRPM4). This compound exhibits significant neuroprotective activity, preventing NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Furthermore, Brophenexin free base has demonstrated protective effects in vivo, safeguarding against brain damage induced by middle cerebral artery occlusion (MCAO) and preserving retinal ganglion cells from NMDA-induced loss. -
TRPML Modulator
TRPML modulator 1 is a selective modulator of the TRPML channel, known for its role in promoting autophagy. With an AC50 of less than 2 mM in the TFEB assay, it effectively enhances autophagic flux, making it a valuable tool for research applications focused on cellular degradation processes and lysosomal function. This compound is instrumental in studying the molecular mechanisms underlying autophagy-related diseases. -
PPARγ/TRPA1 Receptor Partial Agonist
Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics. -
PPAR Agonist
20-HEPE is a metabolite of eicosapentaenoic acid that functions primarily as a peroxisome proliferator-activated receptor α (PPARα) agonist. At a concentration of 10 μM, it effectively activates PPARα in COS-7 cells that express a luciferase reporter gene. Additionally, 20-HEPE activates the mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro, although it does not exhibit analgesic effects in rat models. This compound has potential applications in the study of metabolic processes and receptor signaling pathways. -
TRPM2 Activator
Adenosine 5′-diphosphoribose sodium is a potent activator of the TRPM2 cation channel, which is permeable to Ca2+. This NAD+ metabolite plays a crucial role in cellular signaling and has been shown to enhance autophagy. It serves as a valuable tool for research investigating calcium signaling pathways and the modulation of autophagy in various biological contexts. -
TRPML1/3 Inhibitor
(rel)-ML-SI3 is a selective inhibitor of TRPML1 and TRPML3, exhibiting IC50 values of 3.1 μM and 28.5 μM, respectively. In contrast, it acts as a potent activator of TRPML2 with an EC50 of 3.3 μM. This compound is valuable for research into the roles of TRPML channels in cellular processes and potential therapeutic interventions in related pathologies. Its specificity for multiple isoforms contributes to its utility in exploring calcium signaling pathways and lysosomal function. -
Anti-Adipogenesic Agent
Petasin is an anti-adipogenesic agent that effectively inhibits adipogenesis in 3T3-F442A cells with an IC50 of 0.95 μM. It achieves this by suppressing the expression of lipid synthesis factors such as ACC1, FAS, and SCD1 through the inhibition of transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels. Additionally, Petasin inhibits mitochondrial complex I, contributing to reduced tumor growth and metastasis. By activating the AMPK signaling pathway, it plays a significant role in the regulation of glucose and lipid metabolism. Petasin is also noted for its oral bioactivity. -
TRPA1 Inhibitor
Aurothiomalate disodium acts as a TRPA1 inhibitor, effectively blocking NF-κB activation and inhibiting iNOS expression. This compound fosters the M2 transformation of macrophages and enhances the expression of TREM-2 and arginase-1. Aurothiomalate disodium is applicable in research concerning liver fibrosis, cirrhosis, and arthritis, providing insights into inflammation and tissue repair mechanisms. -
Stable Isotope
Probenecid-d14 is a deuterated form of Probenecid, which serves as a selective agonist of the transient receptor potential vanilloid 2 (TRPV2) channels. This stable isotope enables precise tracking and quantification in metabolic studies. Additionally, Probenecid-d14 is recognized for its inhibitory effects on pannexin 1 channels, making it a valuable tool for investigating cellular signaling pathways and receptor interactions in various biological research applications. -
TRPV2 Agonist
Probenecid sodium is the sodium salt form of Probenecid, functioning as a selective agonist for the transient receptor potential vanilloid 2 (TRPV2) channel. This compound has been shown to activate TRPV2, contributing to various physiological responses. Additionally, Probenecid sodium inhibits the pannexin 1 channel, making it valuable for studying cellular communication and inflammation processes. Its utility in research extends to investigating the role of TRPV2 in pain sensation and other biological pathways. -
MT1/MT2 Receptor Agonist
Piromelatine is a selective agonist for the melatonin MT1 and MT2 receptors, alongside its activity as a serotonin 5-HT1A/5-HT1D agonist and a 5-HT2B antagonist. This compound exhibits various biological activities, including promoting sleep, providing analgesic effects, and demonstrating anti-neurodegenerative, anxiolytic, and antidepressant properties. Additionally, Piromelatine shows inhibitory effects on pain-associated channels such as P2X3, TRPV1, and Nav1.7, making it a valuable tool for research in neuropharmacology and pain management. -
PTHR/PKCα/β Activator
pTH-Related Protein (1-40) is an activator of the parathyroid hormone receptor (PTHR) and protein kinase C isoforms α and β. This peptide enhances calcium uptake in rat intestinal cells by stimulating the PTHR1 receptor, leading to the upregulation of critical calcium transport proteins, including TRPV6, CaBP-D9k, NCX1, and PMCA1. Its biological activity makes it a valuable tool for research focused on calcium signaling and endocrine regulation in both human and animal models.
