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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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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 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. -
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. -
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. -
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. -
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. -
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. -
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. -
TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. -
TRPC6 inhibitor
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected. -
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. -
TRPC6 inhibitor
DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM. -
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. -
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. -
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. -
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. -
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. -
TRPV3 Inhibitor
Trpvicin is a selective inhibitor of the TRPV3 channel, demonstrating IC50 values of 0.41 μM and 0.22 μM for human TRPV3-WT and the hTRPV3-G573S mutant, respectively. Its mechanism of action involves stabilizing TRPV3 in a closed conformation primarily through VSLD-PD binding, while also engaging alternative binding sites in the G573S mutant to impede channel activity. Trpvicin exhibits minimal off-target effects on other TRP family members, making it a valuable tool for studying inflammation, immunology, and conditions associated with itch and hair loss in mouse models. -
TRPM3 Inhibitor
TRPM3-IN-1 is a potent inhibitor of the TRPM3 ion channel, exhibiting an IC50 value of less than 1 µM. This compound is valuable for research focused on the modulation of pain mechanisms and inflammatory responses. Its ability to selectively target TRPM3 makes it a promising tool for investigating related biological pathways and potential therapeutic applications. -
TRPML1/2/3 Inhibitor
(1R,2R)-ML-SI3 is a selective inhibitor of the TRPML1, TRPML2, and TRPML3 ion channels, with IC50 values of 1.6 μM, 2.3 μM, and 12.5 μM, respectively. This compound is valuable for investigating the physiological roles of TRPML channels in cellular signaling and ion homeostasis. It is well-suited for research applications related to lysosomal function, calcium signaling, and potential therapeutic strategies targeting lysosomal storage disorders. -
TRPM4 Inhibitor
TRPM4-IN-2 is a potent inhibitor of the transient receptor potential melastatin 4 (TRPM4) channel, exhibiting an IC50 value of 0.16 µM. This compound is particularly relevant in the study of prostate and colorectal cancers, providing valuable insights into TRPM4's role in tumor biology and potential therapeutic pathways. Its ability to modulate TRPM4 activity makes it a useful tool in cancer research and drug development. -
TRPV1/A1 Inhibitor
Resolvin D2 is a potent TRPV1 and TRPA1 inhibitor with a primary mechanism targeting these transient receptor potential channels in primary sensory neurons. As a metabolite of docosahexaenoic acid (DHA), it exhibits significant anti-inflammatory and anti-infective properties, effectively regulating leukocyte function and controlling microbial sepsis. This compound's high potency and specificity make it a valuable tool in research focused on pain modulation and inflammatory responses. -
TRPM4 Inhibitor
TRPM4-IN-1 is a selective inhibitor of the TRPM4 ion channel, exhibiting an IC50 value of 1.5 μM. This compound is primarily utilized in studies related to cardiac diseases and prostate cancer, facilitating insights into the role of TRPM4 in these conditions. Its potency makes it a valuable tool for investigating the modulation of calcium signaling pathways in various biological contexts. -
TRPA1 Inhibitor
AP-18 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1), effectively blocking TRPA1 activation by 50 µM cinnamaldehyde with IC50 values of 3.1 µM for human and 4.5 µM for mouse TRPA1. This compound demonstrates significant analgesic properties, as it reverses complete Freund's adjuvant-induced mechanical hyperalgesia in murine models. Additionally, AP-18 significantly reduces AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 µM, making it a valuable tool for research into pain mechanisms and TRPA1-related pathways. -
TRPM7 Inhibitor
VPC01091.4 is a potent TRPM7 inhibitor that effectively blocks TRPM7 current at low micromolar concentrations. This compound is capable of crossing the blood-brain barrier, making it suitable for neurological studies. Additionally, VPC01091.4 demonstrates significant anti-inflammatory properties, halting systemic inflammation in vivo, and can be utilized in research focused on inflammation and neuronal signaling pathways. -
TRPA1 Inhibitor
BAY-390 is a selective TRPA1 inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent inhibitory activity with IC50 values of 16 nM for human TRPA1 (hTRPA1) FLIPR, 82 nM for hTRPA1 electrophysiology (Ephys), 63 nM for rat TRPA1 (rTRPA1) FLIPR, and 35 nM for rat dorsal root ganglion (DRG) Ephys. BAY-390 is suitable for investigating the role of TRPA1 in inflammation-related research. -
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.
