Catalog No.
Product Name
Application
Product Information
Citations
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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. -
FRα Modulator
Ricorfotide vedotin is a dual-ligand peptide-drug conjugate that primarily targets Folate receptor α (FRα) while also binding to TRPV6. It exhibits high-affinity binding to FRα and low-affinity interaction with TRPV6, demonstrating notable antitumor activity. This reagent is applicable in advanced solid tumor research, including studies focused on colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma. -
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. -
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. -
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. -
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. -
δ2-opioid Receptor Antagonist/TRPM7 Activator
Naltriben mesylate is a potent antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It demonstrates high affinity, with Ki values of 0.013 nM for the δ receptor, alongside 19 nM and 152 nM for μ and κ receptors, respectively. Research indicates that Naltriben mesylate enhances glioblastoma cell migration and invasion, making it a valuable tool for studies related to neurological diseases and cancer biology. -
TRPV1 Antagonist/MOR Agonist
TRPV1 Antagonist 11 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 29.3 nM. Additionally, it serves as a μ-opioid receptor (MOR) agonist with a Ki value of 60.3 nM. This compound demonstrates significant analgesic properties by antagonizing TRPV1, thereby reducing pain signaling, and activating MOR, which enhances the pain-relief effect. TRPV1 Antagonist 11 has been shown to provide a robust, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice, making it a valuable tool for pain research. -
δ2-opioid Receptor Antagonist/TRPM7 Activator
Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas. -
OT Receptor Agonist
(Thr4,Gly7)-Oxytocin is a specific agonist of the oxytocin receptor (OT receptor). This analogue enhances neuronal excitability in subicular neurons through the activation of TRPV1 channels and the inhibition of K+ channels. Its unique properties make it valuable for research applications involving neurobiology and the study of oxytocin-related pathways. -
TRPV1 Inhibitor
(±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels. -
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. -
TRPA1 Channel Antagonist
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain. -
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 Agonist
ML-SA5 is a potent agonist of the TRPML1 cation channel, effectively activating the endosomal TRPML1 current in DMD myocytes with an EC50 of 285 nM. This compound demonstrates significant anticancer activity by inhibiting tumor growth, making it valuable for research applications aimed at exploring TRPML1 functions and their implications in cancer biology and muscle disorders. -
TRPC Agonist
IA-Alkyne is a TRPC channel (TRPC) agonist that facilitates the investigation of respiratory infections through enhanced channel activity. This compound serves as a versatile chemical probe for quantitative profiling of cysteine reactivity, enabling isotopic tagging. Additionally, IA-Alkyne features an alkyne functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in various biological research studies. -
TRPM3 Agonist
CIM0216 is a selective agonist of the TRPM3 ion channel, demonstrating potent stimulation specifically for this target over other TRPM family members such as TRPM1, TRPM2, and TRPM4-8. It activates TRPM3-dependent pathways to induce pain and facilitate the release of neuropeptides from sensory nerve terminals in vitro. This compound serves as an important research tool for investigating the physiological roles of TRPM3 and has applications in the study of neurogenic inflammation. -
TRPC6 Antagonist
BI-749327 is a potent and highly selective antagonist of the TRPC6 channel, exhibiting IC50 values of 13 nM for mouse TRPC6, 19 nM for human TRPC6, and 15 nM for guinea pig TRPC6. This compound demonstrates an 85-fold selectivity for mouse TRPC6 over TRPC3 and a 42-fold selectivity over TRPC7. Due to its oral bioavailability and inhibition of TRPC6, BI-749327 is suitable for research applications involving ion channel modulation and the investigation of associated physiological and pathological processes. -
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. -
TRPV2 Antagonist
SET2 is a selective antagonist of the TRPV2 channel, with an IC50 value of 0.46 μM. This compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. Additionally, SET2 diminishes lysophosphatidic acid (LPA)-induced increases in cytoplasmic calcium levels, making it useful for research focused on cancer biology and calcium signaling pathways. -
TRPV4 Antagonist
GSK205 is a selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4) channel, exhibiting an IC50 of 4.19 μM for TRPV4-mediated calcium influx inhibition. This compound is instrumental in studying TRPV4's role in various physiological and pathological processes, including pain sensation, inflammation, and cellular mechanotransduction. GSK205 is a valuable tool for researchers investigating the therapeutic potential of TRPV4 modulation in various disease models. -
TRPM2 Inihibitor
JNJ-28583113 is a potent TRPM2 inhibitor that exhibits permeability across the blood-brain barrier. By inhibiting TRPM2, JNJ-28583113 effectively blocks the phosphorylation of GSK3α and β subunits, offering protective effects against oxidative stress-induced cell death. Additionally, it reduces cytokine release from microglia in response to pro-inflammatory stimuli, making it a valuable tool for research in neuroinflammation and oxidative stress pathways. -
TRPM8 Channel Blocker
AMTB hydrochloride is a selective antagonist of the TRPM8 channel, effectively inhibiting icilin-induced TRPM8 activation with a pIC50 of 6.23. This reagent is valuable in the study of overactive bladder conditions and painful bladder syndrome. Additionally, AMTB hydrochloride exhibits non-selective inhibition of voltage-gated sodium channels, providing a broader context for its use in electrophysiological research. -
TRPC3 Agonist
GSK1702934A is a selective agonist of the TRPC3 ion channel. It enhances cardiac contractility and plays a role in the modulation of arrhythmogenesis through TRPC3 activation. This compound is valuable for research applications investigating cardiac function and the physiological effects of TRPC3 modulation in various disease models. -
TRPA1/TRPV1 Agonist
Hydroxy-α-sanshool is an agonist of the transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) channels, exhibiting EC50 values of 69 μM and 1.1 μM, respectively. This compound plays a significant role in pain research by activating these nociceptive pathways, potentially contributing to studies on pain sensation and modulation. -
TRPC4/5 Activator
Englerin A is a selective activator of TRPC4 and TRPC5 channels, exhibiting EC50 values of 11.2 nM and 7.6 nM, respectively. This compound is known to induce cell death in renal carcinoma cells through the mechanism of increased calcium influx and subsequent calcium overload. Englerin A serves as a valuable tool for investigating TRPC channel function and potential therapeutic approaches in cancer research. -
RARβ/RARα Antagonist
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts. -
TRPV2 Blocker
TRPV2-selective blocker 1 is a selective inhibitor of the transient receptor potential vanilloid 2 (TRPV2) channel, exhibiting an IC50 of 6.3 μM. This compound selectively targets TRPV2 without affecting TRPV1, TRPV3, or TRPV4 channels. Its primary biological activities include blocking TRPV2-mediated Ca2+ influx in macrophages and inhibiting macrophage phagocytosis, making it a valuable tool for research on immune responses and cellular signaling pathways involving TRPV2. -
TRPML1 Agonist
MK6-83 is a potent agonist of TRPML1, exhibiting enhanced efficacy and activity. This compound exhibits potential for research into Mucolipidosis type IV, facilitating investigations into the physiological role of TRPML1 and its implications in related pathologies. Its use may contribute to a deeper understanding of lysosomal function and associated 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. -
TRPA1 Channel Activator
Umbellulone is a potent TRPA1 channel activator derived from the leaves of Umbellularia californica. This compound selectively stimulates TRPA1 channels in peptidergic, nociceptive neurons, thereby activating the trigeminovascular system. Umbellulone is valuable for research applications focused on pain signaling pathways and the mechanisms underlying migraine and other pain-related disorders. -
TRPV1 Activator
N-Oleoyldopamine is an oral TRPV1 activator and 5-lipoxygenase (5-LOX) inhibitor that effectively crosses the blood-brain barrier. It stimulates histaminergic neurons in the tuberomammillary nucleus via a dopamine receptor mechanism, independent of TRPV1 and cannabinoid receptors. N-Oleoyldopamine enhances insulin release and promotes glucose-dependent insulinotropic polypeptide through a GPR119-dependent pathway, thus improving glucose tolerance. Additionally, it benefits cardiovascular health by mitigating left ventricular dysfunction and reducing myocardial infarction size through the release of substance P and calcitonin gene-related peptide. This compound is valuable for research into glycemic control and myocardial ischemia-reperfusion injury. -
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. -
TRPV1 siRNA
Tivanisiran sodium is a small interfering RNA (siRNA) that targets the mRNA of transient receptor potential vanilloid 1 (TRPV1). It is primarily utilized in the research of dry eye disease by effectively silencing TRPV1 expression, which is involved in pain and sensory signaling. This agent facilitates the exploration of TRPV1's role in ocular conditions, contributing to the development of potential therapeutic strategies for managing dry eye symptoms. -
TRPA1 Agonist
ASP7663 is a potent and selective agonist of the transient receptor potential ankyrin 1 (TRPA1) channel. Its pharmacological profile indicates significant biological activity in alleviating constipation and reducing abdominal pain. ASP7663 serves as a valuable tool for research into gastrointestinal disorders and the modulation of nociceptive pathways. -
TRPA1 Agonist
Moringin is a potent and selective natural agonist of the TRPA1 ion channel, exhibiting an EC50 value of 3.14 μM. It demonstrates minimal activation of vanilloid channels TRPV1, TRPV2, TRPV3, and TRPV4, as well as the cooling receptor TRPM8. Moringin is associated with various biological activities, including hypoglycemic, antimicrobial, anti-inflammatory, anticancer, and neuroprotective effects, making it valuable for research applications in these areas. -
TRPC5 Activator
BTD is a selective activator of the transient receptor potential canonical 5 (TRPC5) channel, known for its roles in neuronal signaling. This compound facilitates the investigation of TRPC5-mediated pathways, making it a valuable tool for research into neurological diseases and related physiological processes. The modulation of TRPC5 activity by BTD can provide insights into therapeutic targets and mechanisms associated with neurodegenerative conditions. -
TRPV6 Antagonist
SOR-C13 is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel implicated in malignancy and poor prognosis in breast cancer. This compound exhibits significant anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. -
TRPM8 Antagonist
PF-05105679 is a selective antagonist of the transient receptor potential melastatin 8 (TRPM8) channel, exhibiting an IC50 of 103 nM. This compound demonstrates promising biological activity in modulating cold-related pain pathways. It is suitable for research applications investigating the role of TRPM8 in nociception and pain management strategies.
