Catalog No.
Product Name
Application
Product Information
Citations
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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. -
DPP8/9 Inhibitor
DPP8/9-IN-2 is a selective inhibitor of dipeptidyl peptidase 8 and 9 (DPP8/DPP9) with potent inhibitory activity, exhibiting IC50 values of 0.22 nM and 3 nM, respectively. This compound has been implicated in research related to tumor biology and other pathological conditions. Notably, DPP8/9-IN-2 demonstrates certain cardiotoxicity, indicated by its IC50 values of 0.7 μM for the hERG potassium channel, 29.0 μM for the Nav1.5 sodium channel, and 27.7 μM for the Cav1.2 calcium channel. -
Stable Isotope
Lansoprazole-d4 is a deuterium-labeled derivative of Lansoprazole, a proton pump inhibitor that inhibits gastric acid secretion by targeting the H+/K+ ATPase in the gastric parietal cells. The incorporation of deuterium enhances the stability and can facilitate metabolic studies and pharmacokinetic research applications. This stable isotope-labeled compound is valuable for tracing studies, improving analysis of drug metabolism, and understanding the pharmacodynamics of proton pump inhibitors. -
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. -
H+, K+-ATPase Inhibitor
Esomeprazole hemistrontium is a potent H+, K+-ATPase inhibitor that functions as an effective proton pump inhibitor. It reduces gastric acid secretion by targeting the H+, K+-ATPase enzyme in parietal cells. This compound is particularly valuable for research applications related to symptomatic gastroesophageal reflux disease. -
Potassium-Competitive Acid Blocker
Vonoprazan hydrochloride is a potassium-competitive acid blocker (P-CAB) that inhibits H+,K+-ATPase activity, exhibiting an IC50 of 19 nM at pH 6.5. Its potent antisecretory effects make it a valuable reagent in research related to acid-related conditions, including gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride is also utilized for studies focusing on the eradication of Helicobacter pylori, contributing to advancements in gastrointestinal therapeutics. -
Na+/K+ ATPase Inhibitor
Chamigrenol is an inhibitor of the Na+/K+ ATPase, exhibiting an IC50 value of 15.9 μg/mL. This compound demonstrates significant antibacterial activity against both Gram-positive and Gram-negative bacteria, with the exception of Escherichia coli, showing minimum inhibitory concentration (MIC) values of 50 µg/mL. Chamigrenol is valuable for research in microbiology and the development of novel antimicrobial agents. -
Na+/K+-ATPase Inhibitor
(-)-γ-Cuparenol is a sesquiterpene compound that acts as an inhibitor of Na+/K+-ATPase, with an IC50 value of 23.6 μg/mL in porcine models. It has demonstrated the ability to reduce phytohemagglutinin (PHA)-induced activation of NF-AT and NF-κB in Jurkat cells, indicating potential applications in immunoregulation. Additionally, (-)-γ-Cuparenol exhibits antibacterial activity against certain Gram-positive and some Gram-negative bacteria, as well as weak inhibitory effects on Candida albicans. This compound is relevant for research exploring cardiovascular diseases and bacterial infections. -
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. -
H+, K+-ATPase Inhibitor
Esomeprazole (S-Omeprazole) is a potent H+, K+-ATPase inhibitor that functions as an effective proton pump inhibitor. It reduces gastric acid secretion by specifically inhibiting the H+, K+-ATPase enzyme in parietal cells of the stomach lining. This compound is valuable in research related to gastroesophageal reflux disease and studies investigating acid secretion mechanisms. -
Potassium Channel Activator
Kaurenoic acid is a diterpene that acts as a potassium channel activator. It exhibits various biological activities, including antibacterial, anti-inflammatory, anticonvulsant, analgesic, and aortic vasodilating effects. This compound is primarily utilized in research related to neuroprotection, cardiovascular health, and the modulation of ion channel activity. -
Calcium Channel Agonist
(2R,3R)-Butane-2,3-diol functions as a reversible agonist of lanthanum-sensitive calcium channels in bacteria, specifically Escherichia coli, with an EC50 of approximately 25 mM. This compound interacts with calcium channel proteins, promoting channel opening and facilitating extracellular calcium influx, which leads to intracellular calcium transients. Such activity plays a crucial role in regulating bacterial physiological processes, including growth, metabolism, and signal transduction. Additionally, (2R,3R)-Butane-2,3-diol is valuable for investigating bacterial-host cell signaling dynamics and studying conditions like lactose intolerance and other related gastrointestinal disorders. -
Proton Pump Inhibitor
(S)-Lansoprazole is a proton pump inhibitor that effectively reduces gastric acid secretion by inhibiting the proton pump in the stomach lining. This compound demonstrates significant potential for therapeutic applications in acid-related gastrointestinal disorders such as gastroesophageal reflux disease (GERD) and peptic ulcers. Additionally, as a neutral sphingomyelinase (N-SMase) inhibitor, it has been investigated for its role in modulating exosome release and may offer insights into neuroprotective research. -
H+, K+-ATPase Inhibitor
Esomeprazole potassium salt is a potent H+, K+-ATPase inhibitor, primarily functioning as a proton pump inhibitor. It effectively reduces gastric acid secretion by targeting the H+, K+-ATPase enzyme in gastric parietal cells. This compound is valuable for research applications focusing on symptomatic gastroesophageal reflux disease and related gastrointestinal disorders. -
Antibiotic
Milbemycin α10 is a macrolide antibiotic that targets glutamate-gated chloride channels in nematodes and arthropods. It exhibits potent insecticidal activity, effectively controlling a variety of agricultural pests, including larvae and other harmful insects. This compound is valuable for research in agricultural biotechnology and pest management. -
Parasite Inhibitor
Milbemycin oxime is an orally active macrolide that serves as a potent inhibitor of parasite activity. This compound, a mixture of oxime derivatives related to milbemycin A4 and A3, selectively binds to glutamate-gated chloride channels, leading to paralysis and death of various intestinal nematodes and lung/heart worms. It is widely utilized in research focused on antiparasitic drug development and mechanisms of parasitic resistance. -
P-gp Inhibitor
Milbemycin A4 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing multidrug resistance in tumor cells. As a member of the macrolide antibiotic family, Milbemycin A4 displays significant insecticidal and acaricidal properties. This compound is valuable for research focused on overcoming chemotherapy resistance and studying P-gp-related mechanisms in cellular drug transport. -
ATPase/Bacterial Inhibitor
Dihydronovobiocin is a bacterial inhibitor that targets ATPase activity by binding to the GyrB subunit of DNA gyrase. This compound is useful for investigating the interactions between coumarin antibiotics, such as Novobiocin, Chlorobiocin, and Coumermycin, and their effects on DNA gyrase function. Dihydronovobiocin also has potential applications in the study of bacterial infections, facilitating research into the mechanisms of antibiotic action and resistance. -
TREK-1 Channel Blocker
Spadin is a potent TREK-1 channel blocker with an IC50 value of 10 nM. This natural peptide, derived from a propeptide released into the bloodstream, enhances 5-HT neurotransmission in the dorsal raphe nucleus of mice, promoting hippocampal CREB activation and neurogenesis. Spadin is valuable for research applications targeting antidepressant mechanisms and neuroplasticity. -
SERT/VMAT2 probe
FFN246 is a fluorescent probe that selectively targets the serotonin transporter (SERT) and vesicular monoamine transporter 2 (VMAT2), exhibiting excitation and emission spectra of 392 nm and 427 nm, respectively. This compound is ideal for labeling serotonergic neurons in mouse brain tissue, facilitating the study of serotonergic signaling and neuronal activity. Its dual substrate properties make FFN246 a valuable tool in neurobiological research and the exploration of neurotransmitter dynamics. -
Dopamine D2/5-HT2A Receptor Antagonist
Spiperone hydrochloride is a potent antagonist of dopamine D2 and 5-HT2A receptors, exhibiting Ki values of 0.06 nM and 1 nM, respectively. In addition, it selectively antagonizes the α1B-adrenoceptor and activates calcium-activated chloride channels (CaCC). This compound has demonstrated significant antipsychotic and anti-inflammatory properties, making it a valuable tool for research in neuropharmacology and inflammation studies. -
Stable Isotope
Chlorpromazine-d6 hydrochloride is a deuterated derivative of Chlorpromazine, primarily functioning as a dopamine receptor antagonist. This stable isotope is utilized in biochemical and pharmacological research to explore the interactions and mechanisms of action of antipsychotic agents. Its ability to inhibit serotonin receptors, potassium channels, and sodium channels makes it valuable for studying neuropharmacology and drug metabolism. -
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. -
Potassium Channel Inhibitor
Naluzotan hydrochloride is a selective potassium channel inhibitor that primarily functions as an amidosulfonamide 5-HT1A agonist, exhibiting an IC50 of approximately 20 nM and a Ki value of 5.1 nM. This compound demonstrates notable activity in modulating neurotransmitter pathways, making it a valuable tool for research into anxiety and depression treatments. Additionally, naluzotan hydrochloride acts as a weak hERG K+ channel blocker with an IC50 of 3800 nM, highlighting its potential relevance in cardiac safety assessments. -
Noradrenalin Reuptake Inhibitor
Beloxepin is a synaptosomal noradrenalin reuptake inhibitor and a 5-HT2 receptor antagonist. It demonstrates selective inhibition with approximately 100-fold lower affinity for other monoamine transporters. Beloxepin exhibits significant antidepressant and analgesic properties, making it useful for research centered on mood disorders 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. -
Antiarrhythmic Agent
HNS-32 is an antiarrhythmic agent that demonstrates vasodilatory effects, providing protective benefits against ischemic and reperfusion arrhythmias in canine hearts. This compound exhibits significant negative chronotropic effects on mammalian ventricular myocardium, highlighting its potential for applications in acute coronary syndrome research. HNS-32 serves as a valuable tool for exploring the mechanisms and treatment options for cardiac arrhythmias. -
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. -
ASK1 Inhibitor
ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications. -
Potassium Channel Opener
Bimakalim is an ATP-sensitive potassium channel opener that induces vasodilation by enhancing potassium ion efflux. This compound has been shown to reduce transmural myeloperoxidase (MPO) activity and mimics ischemic preconditioning effects, leading to decreased infarct size and modulation of adenosine release and neutrophil function. Bimakalim is valuable for research applications focused on cardiovascular physiology and ischemia-reperfusion injury studies. -
8,9-Z-isomer of Abamectin B1a
8,9-Z-Abamectin B1a is the 8,9-Z isomer of Abamectin B1a, a key antiparasitic agent. It effectively paralyzes nematodes by interacting with glutamate-gated chloride channels, leading to increased permeability of cell membranes and subsequent paralysis. This compound is widely utilized in research related to parasitology and therapeutic development for nematode infections. -
Antiparasitic Agent
Avermectin A1a is a potent antiparasitic agent that primarily targets nematodes and arthropods. It binds to glutamate-gated chloride channels, effectively blocking nerve signal transmission, which leads to paralysis of the parasites. Avermectin A1a is valuable for research on parasitic infections and contributes to the understanding of mechanisms involved in parasitic control. -
Insecticide
Avermectin B2a is an insecticide that targets glutamate-gated chloride channels (GluCls). Its primary mechanism induces hyperpolarization in nematode and insect neurons, leading to paralysis and mortality. This compound is relevant for research into the control of agricultural pests and the exploration of neurotoxic mechanisms in pests. -
Antiparasitic Agent
Δ2-Avermectin B1a is an antiparasitic agent that targets glutamate-gated chloride channels (GluCls) in the neuromuscular systems of invertebrates. By enhancing chloride ion influx, it induces hyperpolarization of the neuromuscular cell membrane, which inhibits neural signal transmission and ultimately results in paralysis and death of parasites. This compound is of significant interest for research applications aimed at controlling agricultural pests. -
Stable Isotope
Flufenamic acid-d4 is a deuterium-labeled derivative of Flufenamic acid, a non-steroidal anti-inflammatory drug. It primarily functions as a cyclooxygenase (COX) inhibitor while also activating AMP-activated protein kinase (AMPK) and modulating various ion channels, including chloride channels and L-type Ca2+ channels. This compound inhibits TEAD2 YBD functionality, affecting YAP-dependent processes such as cell migration and proliferation. Flufenamic acid-d4 is thus a valuable tool for studies in inflammation, cell signaling, and cancer research. -
Parasite
Doramectin monosaccharide, an acid degradation product of Doramectin, targets glutamate- and GABA-gated chloride channels in nematodes, enhancing their opening and resulting in effective anthelminthic activity. This compound is useful for studying the pharmacodynamics of anthelmintics and exploring mechanisms of resistance in parasitic infection research. Its significance lies in its role in understanding the biochemical pathways involved in nematode neuromuscular function and development. -
hERG Inhibitor
GSK369796 is a selective inhibitor of the hERG potassium ion channel, demonstrating an IC50 value of 7.5 μM. This compound exhibits significant antimalarial activity, making it a valuable tool for research in both cardiac function and malaria therapeutics. Its potential implications in pharmacology and drug development provide a basis for further exploration in ion channel regulation and associated biological pathways. -
Parasiticide
Sisapronil is a phenylpyrazole compound that functions as an ectoparasiticide by inhibiting the GABA-gated chloride channels in parasites, leading to paralysis and death. It exhibits potent activity against a variety of ectoparasites, making it valuable in veterinary medicine for controlling infestations. This compound is utilized in research to investigate mechanisms of action against parasitic infections. -
Cytochrome P450 Inhibitor
Kushenol K is a flavonoid antioxidant derived from the roots of Sophora flavescens, functioning as a selective inhibitor of cytochrome P450 3A4 (CYP3A4) with a Ki value of 1.35 μM. This compound exhibits weak antiviral activity against herpes simplex virus type 2 (HSV-2) with an EC50 of 147 μM. Additionally, Kushenol K inhibits sodium-glucose co-transporters SGLT1 and SGLT2, making it relevant for research in metabolic disorders and viral infections. -
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. -
Glycoside
Bacopasaponin C is a natural glycoside with demonstrated inhibitory effects on P-glycoprotein (P-gp) ATPase activity, showing an IC50 of 57.83 μg/mL in the presence of Verapamil. Isolated from Bacopa monniera, Bacopasaponin C exhibits notable antitumor properties against sarcomas and displays antiparasitic activity against Leishmania donovani. This compound is of interest for research into cancer therapeutics and antiparasitic drug development. -
Anti-malaria Agent
Quinine hemisulfate hydrate, an alkaloid obtained from the bark of the cinchona tree, functions primarily as an anti-malaria agent. It acts as a potassium channel inhibitor, specifically targeting the Slo3 (KCa5.1) channel, and can effectively inhibit channel currents in wild-type mouse models. Its inhibitory activity is quantified with an IC50 value of 169 μM, making it a valuable compound for research into malaria treatment and the modulation of potassium channels. -
Antiparasitic Agent
Tigolaner is an antiparasitic agent that targets γ-aminobutyric acid (GABA) and glutamate-gated chloride channels. This compound exhibits significant antiparasitic activity, making it valuable for research on parasitic infections. Its mechanism of action disrupts neurotransmission in parasites, which can aid in the development of novel therapeutic strategies. -
Sodium Channel Agonist
Cevadine is a voltage-sensitive sodium channel agonist that exhibits insecticidal activity. This compound acts by enhancing sodium ion influx through channels, leading to disruption of neuromuscular function in target organisms. Cevadine is valuable for research in neurobiology and agricultural sciences, particularly in studying sodium channel dynamics and developing pest control strategies. -
Antiparasitic
Modoflaner is an isophenylamide compound that primarily targets gamma-aminobutyric acid-gated chloride channels, functioning as a powerful antiparasitic agent. It demonstrates significant insecticidal activity by allosterically modulating these channels, leading to increased neuronal excitability and paralysis in target pests. This compound is widely utilized in research focused on insect control and parasitic disease management. -
Anti-parasitic Agent
Umifoxolaner is a γ-aminobutyric acid (GABA) regulated chloride channel antagonist with potent anti-parasitic properties. This compound is primarily utilized in research applications targeting parasitic infections, showcasing its potential in controlling and managing various parasitic diseases. The mechanism of action involves interference with chloride ion flow, contributing to the disruption of parasitic neuronal signaling. -
Stable Isotope
Endoxifen-d5 (Z-isomer) is the stable isotope-labeled derivative of the Z-isomer of Endoxifen. This metabolite of Tamoxifen exhibits significant anti-estrogenic activity in breast cancer cells that express the estrogen receptor alpha (ERα), contributing to its therapeutic efficacy in estrogen-sensitive tumors. Additionally, Endoxifen (Z-isomer) demonstrates a concentration-dependent inhibition of the hERG potassium channel, with an IC50 value of 1.6 μM, making it a valuable tool for research into breast cancer treatment and associated cardiotoxic effects. -
Antimalarial Agent
Halofantrine is an antimalarial agent that primarily targets Chloroquine-resistant strains of Plasmodium falciparum. This compound exhibits high lipophilicity and effectively blocks HERG potassium channels, contributing to its pharmacological profile. Halofantrine is utilized in research focused on malaria treatment and the mechanisms of drug resistance in parasitic infections. -
Parasite Inhibitor
Ep vinyl quinidine, an epi-vinyl stereoisomer of Quinidine, serves as a targeted inhibitor of parasitic activity. This compound exhibits significant potential in malaria research, leveraging its capabilities as a selective cytochrome P450db inhibitor. Additionally, it functions as a potassium channel blocker with an IC50 of 19.9 μM, positioning it as a valuable tool for investigating anti-parasitic mechanisms and therapeutic interventions.
