Catalog No.
Product Name
Application
Product Information
Citations
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TRPC1/4/5 channels inhibitor
Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.- Aki Teranishi, .et al. , Nat Commun, 2024, Dec 12;15(1):10476 PMID: 39668169
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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(9):1444-1455 PMID: 41033978
- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(6):932-940 PMID: 40582844
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TRPA1 channel blocker
A 967079 is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively).- L Jin, Z Xie, .et al. , Am J Physiol Heart Circ Physiol, 2023, Dec 1;325(6):H1446-H1460 PMID: 37889254
- L Jin, .et al. , Toxicol Appl Pharmacol, 2021, Jul 13;426:115647 PMID: 34271065
- L. Jin, .et al. , Toxicology and Applied Pharmacology, 2020, 398(1), PMID: 32320793
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MSCs Inhibitor
GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.- Shota Inoue, .et al. , Bone, 2023, Dec:177:116916 PMID: 37777037
- Jean-Baptiste Cavin, .et al. , J Physiol, 2023, Apr;601(7):1183-1206 PMID: 36752210
- Yong Chen, .et al. , Gastroenterology, 2021, Apr 2 PMID: 33819485
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TRPV1 antagonist
AMG 517 is a potent and selective TRPV1 antagonist.- Thieu X Phan, .et al. , J Physiol, 2022, Apr;600(7):1651-1666 PMID: 35020949
- Jun Hai, .et al. , Biosci Biotechnol Biochem, 2020, Jul 7;1-7 PMID: 32633621
- Hai J, .et al. , Biomed Res, 2018, 39(6):279-286 PMID: 30531157
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TRP agonist
Evodiamine is a chemical extracted from the Tetradium family of plants. It acts primarily as a thermogenic and stimulant. -
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. -
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. -
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. - 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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
TRPML Modulator
ML-SI3 is a modulator targeting TRPML1 and TRPML2 channels, exhibiting inhibitory activity with IC50 values of 4.7 μM and 1.7 μM, respectively. This compound effectively inhibits lysosomal calcium efflux and impairs TRPML1-mediated autophagy pathways. Additionally, the components of ML-SI3 serve as activators for TRPML2, with EC50 values of 3.3 μM and 9.4 μM, making it a valuable tool for studying TRPML channel dynamics and their roles in cellular processes. -
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. -
TRPV1 siRNA
Tivanisiran is a small interfering RNA (siRNA) targeting the transient receptor potential vanilloid 1 (TRPV1) mRNA. It is primarily used in research focused on dry eye disease, facilitating the study of TRPV1's role in ocular inflammatory responses. By silencing TRPV1 expression, Tivanisiran enables the investigation of therapeutic strategies aimed at alleviating symptoms associated with dry eye disorders. -
CB1 and TRPV1 agonist
N-Arachidonyldopamine is a selective agonist of the CB1 and TRPV1 receptors, exhibiting a Ki value of 250 nM for the CB1 receptor and an EC50 of approximately 50 nM for TRPV1. This compound plays a significant role in modulating pain and inflammatory responses, making it a valuable tool for research investigating endocannabinoid signaling pathways and their implications in various physiological processes. -
CB1 Agonist
(R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays. -
VR1/CB1 Agonist
OMDM-6 is a hybrid agonist targeting vanilloid receptor type 1 (VR1, TRPV1) with an EC50 of 75 nM and cannabinoid receptor type 1 (CB1) with a Ki of 3.2 μM. This compound also inhibits the cellular uptake of anandamide, demonstrating a Ki of 7.0 μM. Due to its dual mechanism of action, OMDM-6 is valuable for research applications exploring pain modulation and the endocannabinoid system. -
Cannabinoid Receptor
CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways. -
CB1 Agonist
CB1/2 agonist 4 serves as a full agonist for the CB1 receptor and a partial agonist for the CB2 receptor, exhibiting EC50 values of 15.09 nM and 1.16 nM, respectively. It demonstrates high affinity for human CB1 and CB2 receptors, with Ki values of 1.1 nM and 4.2 nM. This compound displays notable antinociceptive activity and effectively activates both cannabinoid and TRPV1 receptors, featuring IC50 and EC50 values of 0.8 μM and 0.12 μM, respectively. CB1/2 agonist 4 is valuable for studies exploring cannabinoid receptor functions and their implications in pain modulation. -
Multi-target modulator
PQM-244 is a multi-target modulator that primarily interacts with TRPV1 and cannabinoid receptors CB1 and CB2. It exhibits noteworthy peripheral antinociceptive properties, effectively addressing both neurogenic and inflammatory pain. Additionally, PQM-244 demonstrates antioxidant activity with an IC50 of 14.15 µM for radical scavenging of DPPH. This compound is suitable for research applications related to chronic pain and inflammatory conditions, including diabetes, atherosclerosis, and Alzheimer's disease. -
β2-Adrenergic Receptor Agonist
Protokylol hydrochloride serves as a potent agonist of the β2-adrenergic receptor. This compound demonstrates significant bronchodilator activity, making it valuable in research related to respiratory function and pulmonary pharmacology. Additionally, it interacts with the TRPV1 receptor, further expanding its potential applications in studying pain pathways and sensory responses. -
TRPV1 Agonist
Protokylol is a TRPV1 agonist that exerts its biological activity through the activation of transient receptor potential vanilloid 1 channels. Its primary application includes functioning as a bronchodilator, which supports airway relaxation and dilation. Research utilizing Protokylol can facilitate investigations into pain modulation, sensory signaling, and respiratory physiology. -
CGRP/TRPV1 Inhibitor
Chrysin 6-C-glucoside 8-C-arabinoside is a potent inhibitor of calcitonin gene-related peptide (CGRP) release and the TRPV1 channel activation. This compound exhibits significant biological activity relevant to nociceptive signaling pathways, making it a valuable tool for anti-migraine research. Its mechanism of action offers insights into potential therapeutic strategies for migraine and related pain disorders. -
Fatty Acid Dopamide
N-Palmitoyl dopamine is a long-chain fatty acid dopamide that interacts with endovaniloids, exhibiting 'entourage' effects on N-arachidonoyl-dopamine (NADA) and anandamide. This compound is not active on the TRPV1 receptor, highlighting its selective profile. N-Palmitoyl dopamine is valuable for research applications focused on cannabinoid and pain signaling pathways, particularly in studies examining the interplay between fatty acid derivatives and endocannabinoid activity. -
TrpAB Inhibitor
BRD-4592 is an allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase (TrpAB), specifically targeting the α-β-subunit interface. It demonstrates potent inhibitory activity, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit. This compound is valuable for research applications aimed at elucidating the role of tryptophan metabolism in tuberculosis and exploring novel therapeutic strategies against Mycobacterium tuberculosis. -
TRPV4 Agonist
4α-Phorbol 12,13-didecanoate is a potent agonist of the transient receptor potential vanilloid 4 (TRPV4). It facilitates calcium ion influx and induces ATP release, thereby serving a role as an osmoreceptor. In animal studies, 4α-Phorbol 12,13-didecanoate has been shown to inhibit water intake and elevate maximal micturition pressure in rats. This compound is valuable for research into inflammation, infection, and the biological mechanisms underlying conditions such as chikungunya virus (CHIKV). -
TRPML Agonist
ML-SA1 is a selective agonist of TRPML channels, promoting lysosomal acidification and enhancing protease activity, which leads to the inhibition of Dengue virus 2 (DENV2) and Zika virus (ZIKV). The compound exhibits IC50 values of 8.3 μM for DENV2 RNA and 52.99 μM for ZIKV RNA. Additionally, ML-SA1 stimulates autophagy, making it a valuable tool for research into broad-spectrum antiviral strategies.
