Catalog No.
Product Name
Application
Product Information
Citations
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P-glycoprotein Inhibitor
P-gp inhibitor 22 is a potent inhibitor of P-glycoprotein (P-gp), effectively blocking its efflux function. This compound has been shown to induce apoptosis and promote the accumulation of MCF-7/ADR cells in the S phase of the cell cycle. Its ability to inhibit P-gp makes it relevant in studies focused on multidrug resistance and cancer therapeutics. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
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. -
HCV Inhibitor
Vedroprevir is a potent inhibitor of the HCV NS3/4A protease, demonstrating an IC50 of 3.2 nM. In addition to its antiviral activity, Vedroprevir also inhibits the breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM, as well as P-glycoprotein (P-gp), MRP1, and MRP2 with IC50 values of 34 μM, 14.9 μM, and 12 μM, respectively. These characteristics make Vedroprevir valuable for research in hepatitis C and multidrug resistance cancer studies. Its favorable pharmacokinetic profile has been observed in preclinical models, including rats and dogs. -
V-ATPase/HIV-1 Inhibitor
Diphyllin is a potent inhibitor of vacuolar H+-ATPase (V-ATPase) with an IC50 of 17 nM, and also acts as an HIV-1 inhibitor with an IC50 of 0.38 μM. This compound effectively disrupts the acidification of osteoclast lysosomes, leading to significant inhibition of osteoclast-mediated bone resorption while leaving osteoblastic bone formation unaffected. Diphyllin is valuable for investigating bone metabolism-related diseases and exploring therapeutic avenues for conditions characterized by excessive bone resorption. -
Stable Isotope
Atazanavir-d5 is a deuterium-labeled derivative of Atazanavir, a highly selective inhibitor of HIV-1 protease. This compound serves as a substrate and inhibitor of the cytochrome P450 enzyme CYP3A4, as well as an inhibitor and inducer of P-glycoprotein (P-gp). Additionally, Atazanavir exhibits activity against SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it valuable for research into HIV and coronavirus-related mechanisms. -
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. -
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. -
Stable Isotope
Atazanavir-d6 is a deuterium-labeled form of Atazanavir, a selective inhibitor of HIV-1 protease. Recognized for its capability as a CYP3A4 substrate and inhibitor, it also exerts dual effects as both an inhibitor and inducer of P-glycoprotein (P-gp). In addition, Atazanavir demonstrates antiviral activity by inhibiting the SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it a valuable tool for research in HIV and coronavirus-related studies. -
ATPase Inhibitor
ATPase-IN-6 is a H+/K+-ATPase inhibitor and a prazole derivative. It exhibits significant antiviral activity against a range of viruses, including HIV-1 and SARS-CoV-2. This compound is useful for research investigating antiviral mechanisms and potential therapeutic strategies for viral infections. -
P-glycoprotein Inhibits
NIK250 is a potent inhibitor of P-glycoprotein, a key mediator of multidrug resistance (MDR) in cancer cells. By disrupting the efflux activity of P-glycoprotein, NIK250 enhances the cellular retention of chemotherapeutic agents, thereby increasing their efficacy. This compound can be utilized in research aimed at overcoming drug resistance in cancer therapies and elucidating the mechanisms of MDR in various pathological contexts. -
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. -
Proton Pump Inhibitor
AHR-9294 is a potent inhibitor of the H+ pump enzyme, specifically targeting H, K-ATPase. This compound effectively inhibits gastric acid secretion in vivo, making it valuable for research related to gastrointestinal physiology and the treatment of acid-related disorders. Its mechanism of action supports studies exploring proton pump inhibition and related therapeutic applications. -
ATPase Inhibitor
Apicularen A is a macrolide that selectively inhibits vesicular ATPases, targeting ATPase activity in cellular processes. This compound has been isolated from the mucoid bacterium Chondrosporium spp. Its potent inhibitory effects make it a valuable tool for research applications focused on cellular transport mechanisms and metabolic regulation. -
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. -
Anti-malarial Agent
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid used primarily as an anti-malarial agent. This compound functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM observed in response to voltage pulses of +100 mV. It is valuable for research applications focused on malaria treatment and investigating ion channel physiology. -
Anti-malaria Agent
Quinine hydrochloride is an alkaloid extracted from the bark of the cinchona tree, primarily functioning as an anti-malarial agent. It acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel and demonstrating inhibitory effects on channel currents evoked by voltage pulses to +100 mV, with an IC50 value of 169 μM. This compound is widely utilized in research applications related to malaria treatment and ion channel studies. -
Anti-malarial Agent
Quinine hemisulfate is an orally active alkaloid derived from cinchona bark, primarily recognized for its anti-malarial properties. This compound acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 value of 169 μM for channel currents induced by voltage pulses to +100 mV. Quinine hemisulfate serves as a valuable reagent for anti-malarial studies and relevant pharmacological investigations.
