Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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. -
Anti-Adipogenesic Agent
Petasin is an anti-adipogenesic agent that effectively inhibits adipogenesis in 3T3-F442A cells with an IC50 of 0.95 μM. It achieves this by suppressing the expression of lipid synthesis factors such as ACC1, FAS, and SCD1 through the inhibition of transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels. Additionally, Petasin inhibits mitochondrial complex I, contributing to reduced tumor growth and metastasis. By activating the AMPK signaling pathway, it plays a significant role in the regulation of glucose and lipid metabolism. Petasin is also noted for its oral bioactivity. -
BRG1/BRM ATPase Inhibitor
BRM/BRG1 ATP Inhibitor-2 is a selective inhibitor of BRG1 and BRM ATPase activity, targeting the SWI/SNF chromatin remodeling complexes. This compound is valuable for investigating the molecular implications of BAF-related disorders, including cancer and developmental syndromes. Its mechanism of action enables researchers to explore the role of ATP-dependent chromatin remodeling in gene expression regulation and cellular differentiation. -
SMARCA2 ATPase Inhibitor
SMARCA2-IN-10 is a selective inhibitor of the SMARCA2 ATPase domain, with an IC50 value of 17.676 μM. This compound has been shown to induce cell death in tumors lacking SMARCA4, making it a valuable tool for investigating SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma. Its targeting of the SMARCA2 ATPase offers significant potential for advancing research in these cancer types. -
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. -
Potassium Fluorescent Indicator
Asante potassium green-2 (TMA) is a cell-impermeable potassium-sensitive fluorescent indicator with an excitation/emission spectrum of 525/545 nm. It selectively detects intracellular potassium ion concentrations, making it valuable for studies involving ion channel activity and cellular signaling. This reagent is essential for investigating potassium homeostasis and its implications in various physiological processes and pathologies. -
Potassium Fluorescent Indicator
Asante Potassium Green-1 (TMA) is a cell-impermeable fluorescent indicator designed to selectively detect potassium ions (K+) with an excitation wavelength of 525 nm and emission wavelength of 545 nm. This compound allows researchers to monitor intracellular potassium levels with high sensitivity and specificity, making it invaluable for studies involving ion transport, cellular signaling, and physiology. Its utility in real-time fluorescence imaging facilitates investigations into potassium's role in various biological processes and disease states. -
Potassium Fluorescent Indicator
Asante potassium green-1 AM is a cell-permeable potassium (K+) sensitive fluorescent indicator with an excitation/emission wavelength of 525/545 nm. This reagent enables the visualization and quantification of potassium ion fluctuations within live cells, making it suitable for studies in neurobiology, cardiac research, and cellular signaling. Its high sensitivity to K+ concentrations facilitates investigations into ion channel activity and cellular excitability, enhancing understanding of various physiological processes. -
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. -
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. -
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. -
Excited-state Intramolecular Proton Transfer Molecules
2-(2′-Hydroxyphenyl)benzimidazole is a well-characterized excited-state intramolecular proton transfer (ESIPT) molecule that demonstrates both normal and tautomer emissions. This compound serves as a valuable fluorescent probe, enabling researchers to explore various biological systems and molecular interactions. Its unique photophysical properties make it an essential tool in studies involving fluorescence spectroscopy and imaging applications. -
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. -
AMPAR Modulator
Nooglutil is a positive modulator of AMPA-type glutamate receptors (AMPARs), enhancing synaptic transmission and plasticity. Additionally, it regulates dopamine D2 receptor function, contributing to its anxiolytic effects. This compound is of significant interest for research into neurodegenerative disorders, including Alzheimer's disease, and offers potential insights into therapeutic strategies targeting glutamatergic and dopaminergic systems. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
Calcium Entry-Blocking
YM-430 is a calcium entry-blocking and beta-adrenoceptor-blocking agent. It effectively inhibits Amifampridine-induced rhythmic contractions with an IC50 value of 59.2 nM and blocks arginine vasopressin-induced ST-segment depression with an IC50 of 36.6 mg/kg. This compound is valuable for research into angina pectoris and related cardiovascular conditions. -
CB1 and TRPV1 agonist
N-Arachidonyldopamine is a selective agonist of the CB1 and TRPV1 receptors, exhibiting a Ki value of 250 nM for the CB1 receptor and an EC50 of approximately 50 nM for TRPV1. This compound plays a significant role in modulating pain and inflammatory responses, making it a valuable tool for research investigating endocannabinoid signaling pathways and their implications in various physiological processes. -
CB1 Agonist
(R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays. -
VR1/CB1 Agonist
OMDM-6 is a hybrid agonist targeting vanilloid receptor type 1 (VR1, TRPV1) with an EC50 of 75 nM and cannabinoid receptor type 1 (CB1) with a Ki of 3.2 μM. This compound also inhibits the cellular uptake of anandamide, demonstrating a Ki of 7.0 μM. Due to its dual mechanism of action, OMDM-6 is valuable for research applications exploring pain modulation and the endocannabinoid system. -
Cannabinoid Receptor
CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways.
