Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
Trimebutine-d5 fumarate is a deuterium-labeled derivative of Trimebutine fumarate, functioning primarily as a multi-target inhibitor and opioid receptor agonist. This compound exhibits key biological activities, including the inhibition of L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa), which regulate calcium influx and potassium efflux. Additionally, Trimebutine-d5 fumarate targets Toll-like receptors, modulating inflammatory signaling pathways, and promotes apoptosis in tumor cells via the AKT/ERK pathway. Its applications are particularly relevant in the study of gastrointestinal disorders, including irritable bowel syndrome (IBS), due to its ability to inhibit excessive smooth muscle contraction. -
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. -
Proton Pump Inhibitor
Revaprazan is a reversible proton pump inhibitor that targets gastric acid secretion. It provides protection to the gastric mucosa and inhibits the degradation of IkappaB-alpha, as well as the inactivation of Akt, leading to a reduction in H. pylori-induced COX-2 expression. This compound is valuable in research applications related to infection and inflammation, particularly in studies of H. pylori-infected gastric inflammation and gastric ulcer pathophysiology. -
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. -
CB1/P-gp Inhibitor
Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR). -
Adenosine reuptake Inhibitor
KF24345 free base is an orally active inhibitor of adenosine uptake. It effectively inhibits adenosine uptake in erythrocytes from humans, mice, rabbits, and hamsters, demonstrating IC50 values of 59.5, 130.1, 104.2, and 30.9 nM, respectively. Additionally, KF24345 free base exhibits anti-inflammatory properties by inhibiting lipopolysaccharide (LPS)-induced production of TNF-α and preventing leukopenia in murine models, making it a valuable tool for research in inflammatory responses and adenosine signaling pathways. -
Progranulin secretion Activator
Progranulin modulator-1 is a selective activator of progranulin (PGRN) secretion. It significantly increases PGRN levels in BV-2 cells and exhibits low cytotoxicity with an EC50 value of 83 nM for PGRN. Additionally, Progranulin modulator-1 inhibits the hERG potassium channel with an IC50 of 3100 nM, making it a valuable tool for research on neuroinflammation and associated neurodegenerative disorders. -
Anti-inflammatory Agent
Siaresinolic acid is an anti-inflammatory compound derived from the leaves of Sabicea grisea. It exhibits significant antinociceptive properties by modulating ATP-dependent potassium channels and inhibiting the influx of leukocytes, plasma leakage, and the production of pro-inflammatory mediators such as TNF-α and IL-1β. Importantly, Siaresinolic acid demonstrates a lack of cytotoxicity in murine macrophages and does not affect locomotor activity even at elevated doses. This compound is suitable for research applications involving pleurisy and pain management. -
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. -
ASK1 Inhibitor
ASK1-IN-11 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of less than 200 nM. This compound also demonstrates inhibitory effects on TNF-α, MYLK/MLCK kinases, and hERG potassium channels. The primary research applications of ASK1-IN-11 include investigations into inflammation-related pathways. -
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. -
Chloride Channel Inhibitor
Shikonin is a potent inhibitor of the TMEM16A chloride channel, exhibiting an IC50 value of 6.5 μM. This compound functions as a specific inhibitor of pyruvate kinase M2 (PKM2) and also modulates inflammatory pathways by inhibiting TNF-α and NF-κB activation. In addition, Shikonin decreases exosome secretion by impairing glycolytic processes and effectively inhibits AIM2 inflammasome activation. Its diverse activities make it a valuable reagent for investigating cellular signaling and inflammatory responses in research applications. -
HIV-1 Entry Inhibitor
Trilobatin is a natural sweetener extracted from Lithocarpus polystachyus Rehd, functioning primarily as an HIV-1 entry inhibitor by targeting the HIV-1 Gp41 envelope protein. It demonstrates neuroprotective effects and acts as a selective SGLT1/2 inhibitor, promoting the proliferation of human hepatoblastoma cells. Trilobatin is valuable for research involving HIV-1 entry mechanisms and potential therapeutic applications in hepatoblastoma and neuroprotection studies. -
V-ATPase Inhibitor
Bafilomycin D is a specific inhibitor of vacuolar-type ATPase (V-ATPase), blocking proton translocation and disrupting acidic environments within cells. This compound exhibits significant antimicrobial, insecticidal, herbicidal, and cytotoxic activities, making it a valuable tool for biochemical research. It is useful in studies related to cellular metabolism, ion homeostasis, and the investigation of V-ATPase functions across various biological systems. -
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. -
Histone Methyltransferase
Lobelane hydrochloride selectively inhibits the vesicular monoamine transporter-2 (VMAT2). This compound demonstrates an affinity for VMAT2 with a K(i) value of 630 nM, while exhibiting low interaction with nicotinic acetylcholine receptors (nAChR). The unique mechanism of action of lobelane hydrochloride makes it a valuable tool for studying neurotransmitter dynamics and offers potential in the development of therapeutic agents aimed at addressing methamphetamine abuse. Its structural analogs may further expand its applications in neuropharmacological research. -
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. -
Calcium Channel Blocker
Nitrendipine is a dihydropyridine calcium channel blocker primarily acting on L-type calcium channels. It exhibits significant antihypertensive properties and has been shown to induce apoptosis in various cellular contexts, including neuroblastoma. Additionally, Nitrendipine alleviates withdrawal symptoms associated with alcohol and morphine and reduces right ventricular hypertrophy and pulmonary vascular alterations induced by intermittent hypoxia. Its diverse biological activities make it valuable in research related to cardiovascular health and cancer biology. -
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. -
Potassium Channel Inhibitor
Dequalinium Chloride is a selective inhibitor of potassium channels sensitive to Apamin. This cationic, lipophilic compound exhibits mitochondrial toxicity and additionally acts as an antagonist of the α7 nicotinic acetylcholine receptor. Dequalinium Chloride demonstrates broad-spectrum antimicrobial properties, exhibiting both bactericidal and fungicidal activities, making it valuable for research in cellular physiology and microbiology. -
Calcium Channel Blocker
Lercanidipine hydrochloride is a third-generation dihydropyridine calcium channel blocker with a primary mechanism of selectively inhibiting vascular calcium channels. Its potent antihypertensive effects are complemented by reno- and neuro-protective properties, making it valuable for research into cardiovascular and neurological conditions. Additionally, Lercanidipine exhibits anti-oxidant, anti-inflammatory, and anti-apoptotic activities, further supporting its utility in various biomedical applications. -
Proton Pump Inhibitor
Pantoprazole sodium is a potent proton pump inhibitor that specifically targets the H+/K+-ATPase enzyme with an IC50 of 6.8 μM. This substituted benzimidazole effectively reduces gastric acid secretion, demonstrating significant anti-secretory and anti-ulcer activities. Additionally, studies indicate that Pantoprazole sodium can enhance tumor growth delay when used in combination with Doxorubicin, making it a valuable tool in cancer research and gastrointestinal studies. -
Antimicrobial Agent
Zinc Pyrithione is an antimicrobial agent primarily known for its antifungal and antibacterial properties, acting by disrupting membrane transport through the inhibition of proton pumps. Additionally, it functions as a copper ionophore, facilitating the delivery of copper ions into cells. This compound serves as a valuable tool in the study of cuproptosis, providing insights into copper metabolism and its implications in various biological 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. -
Mdr1p Inhibitor
P-gp-IN-34 is a potent inhibitor of the Mdr1p pump, targeting multidrug resistance in various biological contexts. It has demonstrated efficacy in inhibiting the yeast-to-hyphal transition in Candida albicans, a critical process in its pathogenicity. This compound is suitable for research applications focused on candidiasis and the mechanisms of antifungal resistance. -
Pma1p-ATPase Inhibitor
ATPase-IN-5 is a potent inhibitor of Pma1p-ATPase, exhibiting an IC50 value of 12.7 μM. This compound is critically important in the study of antifungal mechanisms, providing insights into yeast cell metabolism and enzyme regulation. ATPase-IN-5 offers valuable applications in antifungal research, enabling the exploration of new therapeutic strategies. -
Sodium Channel Inhibitor
Lamotrigine-13C3 is a stable isotope-labeled derivative of Lamotrigine, a highly effective sodium channel inhibitor. This compound selectively targets voltage-gated Na+ channels, leading to stabilization of presynaptic neuronal membranes and a subsequent reduction in glutamate release. Lamotrigine-13C3 is suitable for research applications related to epilepsy, focal seizures, and other neurological disorders. -
Stable Isotope
Omeprazole-d3-1 is a deuterium-labeled form of Omeprazole, a proton pump inhibitor (PPI) primarily targeting acid-related gastrointestinal disorders. This compound exhibits competitive inhibition of CYP2C19, with a Ki ranging from 2 to 6 μM, and has demonstrated antimicrobial effects against both Gram-positive and Gram-negative bacteria. Additionally, Omeprazole acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome production in cell studies. This stable isotope is a valuable tool for pharmacokinetic and metabolic research applications. -
Stable Isotope
Desethyl Amiodarone-d4 hydrochloride is a deuterium-labeled analog of Desethylamiodarone hydrochloride, a significant active metabolite of the antiarrhythmic drug Amiodarone. This compound predominantly arises from the metabolic activity of CYP3A isoenzymes. Desethylamiodarone hydrochloride demonstrates potent inhibition of ATP-sensitive potassium channels, with an IC50 value of 19.1 μM, making it a valuable tool for research in cardiac electrophysiology and drug metabolism studies. -
TRPML Modulator
TRPML modulator 1 is a selective modulator of the TRPML channel, known for its role in promoting autophagy. With an AC50 of less than 2 mM in the TFEB assay, it effectively enhances autophagic flux, making it a valuable tool for research applications focused on cellular degradation processes and lysosomal function. This compound is instrumental in studying the molecular mechanisms underlying autophagy-related diseases. -
Stable Isotope
Diazoxide-d3 is a deuterium-labeled derivative of Diazoxide, an ATP-sensitive potassium channel activator. This compound is primarily utilized in research to investigate insulin regulation and has potential applications in the treatment of hyperinsulinism. Its unique isotopic labeling allows for enhanced tracking and analysis in various biochemical studies. -
Stable Isotope
Omeprazole-d6 is a deuterium-labeled form of Omeprazole, a proton pump inhibitor (PPI) primarily targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) ranging from 2 to 6 μM, making it a valuable tool in drug metabolism studies. In addition to its role in gastrointestinal health, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and serves as a potent inhibitor of neutral sphingomyelinase (N-SMase), thereby impacting exosome production and release. This stable isotope variant is useful for pharmacokinetic studies and tracing in biological research applications. -
ATX Inhibitor/PPARγ Agonist
EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD). -
PPARγ/TRPA1 Receptor Partial Agonist
Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics. -
PPAR Agonist
20-HEPE is a metabolite of eicosapentaenoic acid that functions primarily as a peroxisome proliferator-activated receptor α (PPARα) agonist. At a concentration of 10 μM, it effectively activates PPARα in COS-7 cells that express a luciferase reporter gene. Additionally, 20-HEPE activates the mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro, although it does not exhibit analgesic effects in rat models. This compound has potential applications in the study of metabolic processes and receptor signaling pathways. -
Kir2.1 Agonist
Tetramisole acts as a selective agonist for the inward rectifier potassium channel Kir2.1, displaying an EC50 of approximately 30 μM. This compound enhances the forward transport of Kir2.1 channels, hyperpolarizing the resting potential and shortening action potential duration, while also inhibiting intracellular calcium overload and PKA signaling. Additionally, Tetramisole exhibits anti-arrhythmic and anti-myocardial remodeling properties. It is valuable in cardiac electrophysiology studies and investigations focused on myocardial ischemia and heart failure. -
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. -
TRPA1 Agonist
Methyl syringate is a selective agonist of the TRPA1 receptor, playing a crucial role in the regulation of food intake and gastric emptying through TRPA1-mediated pathways. Additionally, this compound functions as an effective phenolic mediator for bacterial and fungal laccases, enhancing their catalytic activities. Methyl syringate serves as a chemical marker in Asphodel monofloral honey and is associated with its antibacterial properties. Furthermore, it has been shown to inhibit aflatoxin production and may contribute to weight suppression, as well as being applicable in research focused on cancer prevention, hypoxia-induced inflammatory response, and tumorigenesis. -
ecto-ATPase Inhibitor
ARL67156 is an inhibitor of ecto-ATPase, specifically targeting NTPDase1 (CD39), NTPDase3, and NPP1. It exhibits weak competitive inhibition with Ki values of 11 µM, 18 µM, and 12 µM for these enzymes, respectively. This compound is useful for studies investigating purinergic signaling and ATP metabolism in various biological contexts, including cell signaling and immune response research. -
Piezo1 Agonist
MCB-22-174 is a deuterated agonist of the Piezo1 mechanosensitive ion channel, exhibiting an EC50 of 6.28 μM. This compound effectively activates the CaMKII/ERK signaling pathway and promotes calcium influx in rat mesenchymal stem cells (rMSCs). MCB-22-174 reduces the expression of chondrogenic markers, such as Comp and Acan, alongside adipogenic markers including Lpl and Fabp4. This reagent has potential applications in enhancing bone quality in models of disuse osteoporosis, making it a valuable tool for research in skeletal health and regenerative medicine. -
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. -
CFTR Modulator
Olacaftor is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator that enhances the function of the defective CFTR protein. It has been shown to improve chloride ion transport, leading to increased hydration of airway surfaces and improved pulmonary function. Olacaftor is primarily utilized in research focused on cystic fibrosis and the development of therapies aimed at restoring CFTR activity. -
Stable Isotope
Tolbutamide-d9 is a deuterated form of Tolbutamide, which primarily targets ATP-sensitive potassium channels. As a first-generation sulfonylurea, it functions as an oral hypoglycemic agent, playing a critical role in glucose regulation. This stable isotope is valuable for metabolic research and isotopic tracing studies, facilitating investigations into pharmacokinetics and the mechanism of action of sulfonylureas. -
CFTR Inhibitor
BPO-27 racemate is a potent cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor, exhibiting an IC50 of 8 nM. This compound has been shown to effectively suppress CFTR activity, making it valuable for research aimed at understanding CFTR-related disorders. BPO-27 racemate can be utilized in studies investigating ion channel regulation and potential therapeutic interventions for cystic fibrosis. -
Stable Isotope
Omeprazole-d3 is a deuterium-labeled variant of Omeprazole, a widely used proton pump inhibitor (PPI) targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) between 2 to 6 μM, and has been shown to inhibit the growth of both Gram-positive and Gram-negative bacteria. This stable isotope is particularly useful for pharmacokinetic studies, metabolic profiling, and investigations into drug-drug interactions involving Omeprazole. -
Stable Isotope
Omeprazole-13C,d3 is a stable isotope-labeled form of Omeprazole, a proton pump inhibitor (PPI) that targets gastric acid secretion. This compound is utilized in pharmacokinetic studies due to its competitive inhibition of CYP2C19 activity, with an inhibition constant (Ki) ranging from 2 to 6 μM. Additionally, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome release. It is a valuable reagent for research in gastrointestinal physiology, drug metabolism, and cellular signaling pathways. -
CFTR Corrector
Tezacaftor-d4 is a deuterium-labeled CFTR corrector that targets the F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) protein. By facilitating the proper trafficking of CFTR to the cell surface, Tezacaftor-d4 enhances functional chloride transport in epithelial cells. This compound is primarily utilized in research focused on developing therapeutic strategies for cystic fibrosis by restoring CFTR activity. -
Stable Isotope
Reserpine-d9 is a deuterated form of Reserpine that serves as an inhibitor of the vesicular monoamine transporter 2 (VMAT2). This stable isotope-labeled compound is valuable for studies in neuropharmacology and metabolism, allowing for precise tracking and quantification of Reserpine interactions in various biological systems. It enables researchers to explore its effects on neurotransmitter release and potential applications in psychiatric and neurological disorders. -
Autophagy Inducer
Desethylamiodarone hydrochloride is a significant active metabolite of Amiodarone, primarily functioning as an autophagy inducer. It is produced through the action of CYP3A isoenzymes and plays a critical role in cellular processes affecting autophagy. This compound is utilized in research applications focusing on cardiovascular pharmacology and cellular stress responses, due to its influence on potassium channels and potential therapeutic implications in arrhythmias.
