Catalog No.
Product Name
Application
Product Information
Citations
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NMDAR/TRPM4 inhibitor
Brophenexin (compound 8) is a potent inhibitor of the interaction interface between NMDA receptors (NMDAR) and TRPM4 channels, exhibiting significant neuroprotective activity. It prevents NMDA-induced excitotoxicity, including cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. In vivo, Brophenexin protects against brain damage in mice subjected to middle cerebral artery occlusion (MCAO) and preserves retinal ganglion cells from NMDA-induced degeneration. These findings support its potential as a therapeutic agent for neurodegenerative diseases and ischemic brain injury. -
HDAC inhibitor
HL23 is a histone deacetylase (HDAC) inhibitor with demonstrated efficacy against hepatocellular carcinoma (HCC). It enhances acetylation at the TXNIP promoter, leading to upregulation of TXNIP expression and modulation of potassium channel activity, ultimately inducing TXNIP-dependent potassium deprivation. HL23 effectively suppresses HCC progression and metastasis, and exhibits a synergistic antitumor effect when combined with Sorafenib, outperforming the combination of Sorafenib and Vorinostat in preclinical models. -
Bone resorption inhibitor
Chicken calcitonin is a peptide hormone involved in the regulation of calcium metabolism. It inhibits bone resorption by suppressing the motility and activity of osteoclasts, as demonstrated in neonatal rat models. This hormone plays a key role in maintaining bone homeostasis and is of interest in bone-related research. -
TNFα/IL-2 Inhibitor
Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles. -
Potassium Channel Inhibitor
Endoxifen Z-isomer hydrochloride is a selective potassium channel inhibitor that acts as a potent metabolite of Tamoxifen, exhibiting over 100-fold increased potency compared to its parent compound. This compound effectively inhibits PKCβ1 kinase activity, leading to decreased phosphorylation of AKT at Ser473 and its substrates, which ultimately promotes apoptosis. Endoxifen Z-isomer hydrochloride demonstrates significant anticancer effects, particularly against hormone-resistant metastatic breast cancer, making it a valuable reagent for cancer research applications. -
Na+/K+-ATPase Inhibitor
Cryptanoside A is a potent Na+/K+-ATPase inhibitor derived from the stems of Cryptolepis dubia. This cardiac glycoside epoxide exhibits significant cytotoxic effects against various cancer cell lines. Additionally, Cryptanoside A enhances the expression of Akt and the p65 subunit of NF-κB, making it a valuable tool for studying cancer biology and the regulatory pathways involved in cell survival and proliferation. -
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. -
Autophagy Inducer
Diazoxide is an ATP-sensitive potassium channel activator that induces autophagy through modulation of cellular ion balance. This compound demonstrates potential therapeutic effects in conditions related to hyperinsulinism. It is commonly utilized in research applications focusing on autophagy pathways and metabolic regulation. -
Kir2.1 Agonist
Tetramisole hydrochloride is a selective inward rectifier potassium channel agonist that primarily targets the Kir2.1 subunit with an EC50 of approximately 30 μM. This compound plays a crucial role in promoting Kir2.1 channel functioning, hyperpolarizing the resting potential, and shortening action potential duration. Additionally, it exhibits effects on intracellular calcium regulation while influencing PKA signaling, contributing to its anti-arrhythmic and anti-myocardial remodeling properties. Tetramisole hydrochloride is valuable for investigations in cardiac electrophysiology, as well as studies focused on myocardial ischemia and heart failure. -
KATP Inhibitor
Tolbutamide is an orally active KATP inhibitor that primarily targets ATP-sensitive potassium channels. It is known to inhibit cell proliferation and stimulate the exocytosis of glucagon, while also reducing fetal lethality in murine models. This compound is utilized in diabetes research to explore mechanisms of insulin secretion and glucose metabolism. -
Proton Pump Inhibitor
Omeprazole sodium is a proton pump inhibitor (PPI) that effectively reduces gastric acid secretion, making it useful in treating acid-related gastrointestinal disorders. In addition to its primary role, omeprazole sodium competitively inhibits CYP2C19 with a Ki value ranging from 2 to 6 μM, which may influence drug metabolism. This compound also displays antibacterial activity against both Gram-positive and Gram-negative bacteria, and it serves as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome production. Its diverse biological activities make it a valuable tool for research in pharmacology and microbiology. -
Calcium Channel Blocker
Dotarizine is a selective calcium channel blocker that functions by inhibiting Ca2+ influx. This compound demonstrates significant antimigraine activity through its modulation of calcium signaling pathways. Additionally, Dotarizine reduces the release of lactate dehydrogenase and exhibits the capacity to block 5-HT receptors, making it a valuable tool for research in neural signaling and migraine pathophysiology. -
Monoamine Transporter Modulator
6-APDB is a monoamine transporter modulator that selectively influences human monoamine transporters while acting as a partial agonist at 5-HT2 family receptors. It demonstrates potent inhibition of norepinephrine and serotonin reuptake, with IC50 values of 0.56 μM for norepinephrine transporters (NET) and 2.3 μM for serotonin transporters (SERT). Additionally, 6-APDB mediates the release of multiple monoamine neurotransmitters, exhibiting a dose-dependent, biphasic locomotor effect in mice. This compound also has potential empathogenic properties along with behavioral effects relevant to research on monoamine signaling and neuropsychopharmacology, with no significant cytotoxicity observed at high concentrations. -
Calcium Channel Blocker
Levemopamil hydrochloride is a calcium channel blocker that effectively penetrates the blood-brain barrier and acts as a 5-HT2 antagonist. This compound exhibits key biological activity in modulating calcium influx, making it valuable for research related to temporary occlusion and various neurological diseases. It serves as a useful tool for studying the effects of calcium channel modulation on neuronal function and pathophysiology. -
Calcium Channel Blocker
Levemopamil is a calcium channel blocker known for its ability to antagonize 5-HT2 receptors. It demonstrates renoprotective properties, particularly in the context of ischemic acute kidney injury. This compound is suitable for research involving ischemic acute renal failure and related nephroprotective studies. -
5-HT(1A/B/D) Receptor Antagonist
GSK-588045 is a potent antagonist of the 5-HT(1A/B/D) receptors, demonstrating a high degree of selectivity for these targets while sparing human ether-a-go-go related gene (hERG) potassium channels. This specificity makes GSK-588045 a valuable tool in the study of neurological disorders, particularly in the context of depression and anxiety research applications. Its unique profile can aid in elucidating the role of serotonin receptors in various neuropsychiatric conditions. -
Calcium Antagonist
Nexopamil is a calcium antagonist that targets Ca2+ channels, as well as 5-HT2, 5-HT1A, 5-HT1C, and dopamine D2 receptors. This compound demonstrates significant vasodilatory and cardioprotective properties, along with the ability to inhibit platelet aggregation. Nexopamil is useful for research focused on conditions such as stable and unstable angina, as well as potentially in studies of peripheral arterial occlusive disease. -
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. -
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. -
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.
