Catalog No.
Product Name
Application
Product Information
Citations
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Dopamine D2 inhibitor
Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
5-HT3 antagonist
Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy. - Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
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Dopamine Receptor Antagonist
Flupentixol dihydrochloride is a potent antagonist of D1 and D2 dopamine receptors, demonstrating significant inhibition of PI3Kα with an IC50 of 127 nM. This compound exhibits anti-proliferative effects on cancer cells and promotes apoptosis, making it a valuable tool in oncology research. Additionally, Flupentixol has applications in studies related to schizophrenia, anxiety, and depression, contributing to the understanding of these complex neuropsychiatric disorders. -
PAR2 Antagonist
ENMD-1068 hydrochloride is a selective antagonist of protease-activated receptor 2 (PAR2). This compound effectively reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling pathways. Additionally, ENMD-1068 hydrochloride demonstrates the ability to inhibit the proliferation of endometrial cells and induce apoptosis in epithelial cells associated with lesions. This reagent is valuable for research applications in endometriosis and liver fibrosis. -
σ2 Receptor Agonist
PB28 dihydrochloride is a potent σ2 receptor agonist, exhibiting high affinity with a Ki of 0.68 nM, and also acts as a σ1 antagonist with a Ki of 0.38 nM. This compound demonstrates significant biological activity by inhibiting electrically evoked twitch responses in guinea pig bladder and ileum, with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride has been shown to modulate SARS-CoV-2-human protein-protein interactions, induce caspase-independent apoptosis, and display antitumor effects, making it a valuable tool for research in neuropharmacology and cancer biology. -
H1-histamine/P2X7 Receptor Antagonist
Oxatomide is a dual antagonist of the H1-histamine receptor and the P2X7 receptor, noted for its oral bioavailability. It exhibits significant antihistaminic, antiallergic, and anti-inflammatory properties, making it a valuable compound for the study of allergic diseases. Researchers can utilize Oxatomide to investigate mechanisms of allergy and inflammation, contributing to potential therapeutic advancements. -
PAR-1 Antagonist
Atopaxar is a selective and reversible antagonist of the thrombin receptor protease-activated receptor-1 (PAR-1). By inhibiting PAR-1 signaling, Atopaxar serves as an effective antiplatelet agent, disrupting platelet activation and aggregation. This compound is valuable for research applications related to atherothrombotic diseases, providing insights into the mechanisms of platelet-mediated thrombosis and potential therapeutic interventions. -
Adenosine Receptor Agonist
N6-Benzyladenosine is an adenosine receptor agonist that demonstrates significant cytotoxic activity. It effectively induces apoptosis in cells and arrests the cell cycle at the G0/G1 phase, making it a valuable tool for studying cell proliferation and death. Additionally, N6-Benzyladenosine inhibits Toxoplasma gondii adenosine kinase, providing insights into its potential applications in antiparasitic research and glioma studies. -
CBR1 Inhibitor
Hydroxy-PP-Me is a selective inhibitor of the cannabinoid receptor type 1 (CBR1) with an IC50 of 759 nM. It effectively inhibits serum starvation-induced apoptosis and enhances the cytotoxic effects of chemotherapeutic agents such as Daunorubicin and Arsenic Trioxide (As2O3) on tumor cells. Hydroxy-PP-Me is a valuable tool for cancer research, particularly in the study of leukemia and related malignancies. -
A1 Adenosine Receptor Agonist
CCPA (2-Chloro-N6-cyclopentyladenosine) is a highly selective agonist for A1 adenosine receptors, demonstrating a Ki value of 0.4 nM. This compound effectively inhibits adenylate cyclase, with an IC50 of 33 nM. CCPA is relevant in studies investigating anti-seizure and cardioprotective effects, making it a valuable tool for research related to seizures and myocardial infarction. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Adrenergic Receptor Antagonist
Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron is a selective α-1A adrenergic receptor agonist primarily utilized for the treatment of urinary incontinence. This compound exhibits key biological activity by enhancing bladder function, thereby mitigating symptoms associated with overactive bladder. Additionally, Dabuzalgron has been shown to provide protection against Doxorubicin-induced cardiotoxicity through the preservation of mitochondrial function, making it relevant in cardiovascular research. -
S1PR1 Antagonist
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 value of 398 nM. This compound is instrumental in studying the role of S1PR1 in various biological processes, including immune modulation and cardiovascular function. W146 TFA is valuable for research applications involving cytokine signaling and cellular proliferation pathways. -
ICMT Inhibitor
UCM-1336 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 of 2 μM. This compound effectively induces mislocalization of endogenous Ras, resulting in decreased Ras activation. UCM-1336 has shown the ability to trigger cell death through autophagy and apoptosis, making it a valuable tool for research in cancer biology and signal transduction pathways. -
5-HT2/D1/D2 Antagonist
Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions. -
mGlu1 Antagonist
LY456236 is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting an IC50 of 0.145 μM for the inhibition of phosphatidylinositol hydrolysis. Additionally, it demonstrates inhibitory activity against EGFR with an IC50 of 0.918 μM. By targeting the MAPK pathway, LY456236 effectively blocks cell proliferation and reverses the anti-apoptotic effects of DHPG. This reagent is suitable for investigations in epilepsy and related neurological research. -
Dopamine Receptors Blocker
Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis. -
Stable Isotope
Carvedilol-d3 is a deuterium-labeled analogue of Carvedilol, functioning primarily as a non-selective β/α-1 adrenergic receptor blocker. It exhibits significant biological activity by inhibiting lipid peroxidation in a dose-dependent manner with an IC50 value of 5 μM. This compound serves as a versatile antihypertensive agent and has potential applications in the treatment of angina and congestive heart failure. Furthermore, Carvedilol-d3 promotes autophagy and is known to inhibit the NLRP3 inflammasome, making it valuable for research involving inflammatory processes. -
5-HT6R Antagonist
PUC-10 is a potent antagonist of the 5-HT6 receptor, exhibiting a Ki value of 14.6 nM and an IC50 of 32 nM. Computational studies indicate that PUC-10 is orally bioactive and capable of penetrating the blood-brain barrier. This compound effectively induces autophagy in SH-SY5Y neuronal cells by inhibiting the mTOR signaling pathway. PUC-10 is ideally suited for studies focused on neurological disorders and related therapeutic strategies. -
Stable Isotope
Trifluoperazine-d3 dihydrochloride is a deuterated derivative of Trifluoperazine, primarily targeting dopamine receptors to exert its antipsychotic effects. This compound is a potent α1-adrenergic receptor antagonist and an effective inhibitor of NUPR1, showcasing anticancer properties. Additionally, it functions as a calmodulin inhibitor and can interfere with P-glycoprotein activity. Trifluoperazine-d3 dihydrochloride is valuable for research applications related to schizophrenia and serves as a reversible inhibitor of influenza virus morphogenesis. -
Stable Isotope
Yangonin-d3 is a deuterium-labeled derivative of Yangonin, acting as a stable isotope. This compound demonstrates binding affinity for the human recombinant cannabinoid CB1 receptor, with an IC50 of 1.79 μM and a Ki of 0.72 μM. Yangonin-d3 is valuable for research applications in cannabinoid receptor studies, enabling the exploration of receptor mechanisms and the development of cannabinoid-based therapeutics. -
Stable Isotope
Carvedilol-d5 is a deuterium-labeled analogue of Carvedilol, a non-selective β/α-1 adrenergic receptor blocker. It exhibits lipid peroxidation inhibition with an IC50 of 5 μM and serves as a versatile antihypertensive agent, showing potential in the treatment of angina and congestive heart failure. Additionally, Carvedilol functions as an autophagy inducer and inhibits the NLRP3 inflammasome, making it relevant for research in inflammatory pathways and cardiovascular health. -
Autophagy Inducer
Cabergoline diphosphate is an ergot alkaloid that acts as an agonist of dopamine D2-like receptors, demonstrating high affinity for D2, D3, and 5-HT2B receptors with Ki values of 0.7, 1.5, and 1.2, respectively. It serves as an autophagy inducer, making it a valuable tool for research focused on cellular processes related to autophagy and neurobiology. This compound is instrumental in studies investigating neurodegenerative diseases and metabolic regulation, providing insights into the role of dopamine receptors in cellular homeostasis. -
Stable Isotope
Dronedarone-d6 hydrochloride is a deuterium-labeled derivative of Dronedarone, serving as a stable isotope for research applications. This compound functions primarily as a class III antiarrhythmic agent, effective in the study of atrial fibrillation (AF) and atrial flutter. Dronedarone-d6 hydrochloride exhibits potent blockade of various ion currents, including potassium, sodium, and L-type calcium currents, and also demonstrates antiadrenergic activity through noncompetitive binding to β-adrenergic receptors. Additionally, it acts as a substrate and moderate inhibitor of the CYP3A4 enzyme, making it valuable for pharmacokinetic studies. -
Stable Isotope
Cabergoline-d6 is a stable isotope-labeled form of Cabergoline, an ergot-derived dopamine D2-like receptor agonist. This compound exhibits high affinity for dopamine receptors D2 and D3, as well as 5-HT2B receptors, with Ki values of 0.7, 1.5, and 1.2 nM respectively. Cabergoline-d6 is utilized in pharmacokinetic studies and metabolic research to investigate the behavior of Cabergoline in biological systems. -
Stable Isotope
Dronedarone-d6 is a deuterium-labeled derivative of the antiarrhythmic agent Dronedarone, primarily targeting various ion channels, including potassium, sodium, and L-type calcium channels. This compound is vital for investigating the mechanisms underlying atrial fibrillation (AF) and atrial flutter, as well as for studying its antiadrenergic properties through its noncompetitive binding to β-adrenergic receptors. In addition, Dronedarone-d6 serves as a substrate and moderate inhibitor of CYP3A4, making it relevant for pharmacokinetic studies in cardiovascular research. -
CB1 Antagonist/PPARα Agonist
OLHHA is a dual CB1 receptor antagonist and PPARα agonist. This compound demonstrates notable activity in inhibiting alcohol intake with an EC50 value of 0.2 mg/kg. Additionally, OLHHA effectively reduces hepatic lipid accumulation and circulating triglyceride levels, exhibiting anti-steatotic properties. Its mechanism and effects make it a valuable tool for research into non-alcoholic fatty liver disease (NAFLD). -
Stable Isotope
Salbutamol-d3 is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. This compound is primarily employed as a stable isotope for metabolic tracing and pharmacokinetic studies. Salbutamol exhibits significant therapeutic effects by relaxing bronchial smooth muscle, making it a valuable tool in research involving asthma and chronic obstructive pulmonary disease. Additionally, it has been identified to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT pathway, highlighting its utility in oncology research. -
Stable Isotope
Salbutamol-d9 acetate is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. This compound is primarily utilized as a stable isotope for research applications, specifically in studying its effects on bronchial smooth muscle relaxation and the β2-adrenergic receptor pathways. Salbutamol has also been implicated in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling cascade, making it relevant for cancer research as well as respiratory studies. -
Stable Isotope
Salbutamol-d9 is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. It is primarily utilized as a stable isotope in biological research, allowing for the precise tracking of Salbutamol's pharmacokinetics and metabolism. Salbutamol is known for its ability to relax bronchial smooth muscle and is widely studied in the context of asthma and chronic obstructive pulmonary disease, as well as its role in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway. -
mGlu5 Receptor NAM
STX107 is a negative allosteric modulator (NAM) of the metabotropic glutamate 5 (mGlu5) receptor, exhibiting a pKi of 8.32. This compound effectively inhibits glutamate-induced calcium mobilization, inositol monophosphate (IP1) accumulation, and ERK1/2 phosphorylation. Additionally, STX107 prevents glutamate-induced mGlu5 internalization, making it a valuable tool for researching mGlu5 receptor signaling pathways and potential therapeutic applications for neurological disorders. -
Antagonist
Peptide E5 is an antagonist that targets the CXCR4/CXCL12 signaling axis. By blocking this interaction, Peptide E5 downregulates CXCR4 expression and inhibits the phosphorylation of key downstream proteins, Akt and Erk, leading to apoptosis in breast cancer cells. Additionally, Peptide E5 suppresses cellular migration and adhesion, as well as the recruitment of endothelial progenitor cells, thereby inhibiting tumor angiogenesis. This peptide is a valuable tool for research related to breast cancer and tumor microenvironment interactions. -
A1/A2A/A2B Adenosine Receptor Antagonist
Adenosine receptor antagonist 7 is a potent triple antagonist of A1, A2A, and A2B adenosine receptors, demonstrating Ki values of 1.5 nM, 0.6 nM, and 21 nM, respectively. It effectively inhibits cAMP production in A2AR-HEK293 cells with an IC50 of 0.8 nM. This compound enhances the infiltration of effector T cells and increases the CD8+/Treg ratio in conjunction with Avelumab. Adenosine receptor antagonist 7 is valuable for cancer research, particularly in the study of colon cancer. -
CXCR4 Antagonist
Peptide R analogue 10 is a potent CXCR4 antagonist, demonstrating enhanced antagonistic activity, specificity, and plasma stability compared to its predecessor, Peptide R. This compound effectively inhibits CXCL12-mediated cell migration, ERK phosphorylation, and CXCR4 internalization. Peptide R analogue 10 is valuable for research applications involving CXCR4 overexpression in models of leukemia and colon cancer. -
Adrenergic Receptor Agonist
Salbutamol adipate is an orally active short-acting β2-adrenergic receptor agonist. It is known to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT pathway. Additionally, Salbutamol adipate is effective in relaxing bronchial smooth muscle, making it a valuable tool for researching bronchospasm associated with asthma and chronic obstructive pulmonary disease. -
Stable Isotope
Salbutamol-d4 is a deuterated form of the beta-2 adrenergic receptor agonist Salbutamol, designed for stable isotope applications in biochemical research. This compound has been shown to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway. In addition, Salbutamol-d4 is utilized in studies investigating bronchospasms associated with asthma and chronic obstructive pulmonary disease (COPD), allowing for precise tracking of biological processes and metabolic pathways. -
DPP4 Inhibitor
Sitagliptin hydrochloride is a selective DPP4 inhibitor, demonstrating an IC50 of 19 nM. By inhibiting DPP4, this compound prevents the breakdown of incretin hormones, such as GLP-1 and GIP, ultimately increasing their active levels. Additionally, sitagliptin can stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, independent of DPP-4 inhibition. This reagent is applicable in research involving type 1 and type 2 diabetes, and it also exhibits protective effects on pancreatic islet grafts in type 1 diabetes models. -
Stable Isotope
Sitagliptin-d6 is a deuterium-labeled derivative of Sitagliptin, a selective DPP-4 inhibitor that demonstrates an IC50 of 19 nM. By inhibiting the degradation of incretins such as GLP-1 and GIP, Sitagliptin-d6 promotes increased levels of active glucagon-like peptides, thereby enhancing insulin secretion in a glucose-dependent manner. Additionally, it can stimulate GLP-1 secretion from intestinal L cells independently of DPP-4 inhibition, engaging the cAMP/PKA and ERK1/2 signaling pathways. This reagent is valuable for research on type 1 and type 2 diabetes, as well as the protective effects on pancreatic islet grafts. -
ICMT Inhibitor
POP-3MB is an inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 2.5 μM. It effectively alters the subcellular localization of K-Ras, leading to inhibition of Ras activation. Additionally, POP-3MB demonstrates the capacity to inhibit Erk phosphorylation, making it a valuable tool for research into Ras signaling pathways and related oncogenic processes. -
GPR119 Agonist
2-Oleoylglycerol is a GPR119 agonist that activates hGPR119 in transiently transfected COS-7 cells with an EC50 value of 2.5 μM. This lipid enhances the inflammatory response in macrophages and promotes fibrosis through the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. Additionally, 2-Oleoylglycerol stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. Its effects make it a valuable tool for research into non-alcoholic steatohepatitis (NASH) and related metabolic disorders. -
Stable Isotope
2-Oleoylglycerol-d5 is a deuterium-labeled derivative of 2-Oleoylglycerol, a known agonist of GPR119. It exhibits significant biological activity by activating human GPR119 with an EC50 of 2.5 μM in COS-7 cells, enhancing macrophage inflammatory responses and promoting fibrosis through the GPR119/TAK1/NF-κB/TGF-β1 signaling cascade. Additionally, this compound stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol-d5 is particularly useful for studying mechanisms underlying non-alcoholic steatohepatitis (NASH). -
S1P2 Receptor Inhibitor
S118 is an orally active inhibitor of the sphingosine-1-phosphate receptor 2 (S1P2 receptor), which blocks the binding of Dpr1, subsequently reducing β-catenin accumulation. This mechanism inhibits nuclear translocation of the S1P2 receptor, contributing to the attenuation of inflammation, fibrosis, and epithelial-mesenchymal transition (EMT). S118 demonstrates potential for use in research related to idiopathic pulmonary fibrosis (IPF) and other fibrotic diseases. -
Bone Marrow Mesenchymal Stem Cell Inducer
Herpetin is an active lignan that functions as a bone marrow mesenchymal stem cell inducer. It activates the SDF-1/CXCR4 axis and the Wnt/β-catenin signaling pathway, promoting stem cell recruitment and differentiation. This compound is relevant for research applications focused on acute liver injury and related regenerative processes. -
Platelet Aggregation Inhibitor
12(S)-HETrE is a fatty acid metabolite that serves as a potent inhibitor of platelet aggregation. This compound demonstrates significant biological activity in modulating thrombus formation and is valuable in thrombosis-related research applications. Researchers can utilize 12(S)-HETrE to study the molecular mechanisms underlying platelet function and explore potential therapeutic targets in cardiovascular diseases. -
Adenosine Receptor Antagonist
Adenosine receptor antagonist 6 selectively targets the A2A adenosine receptor, exhibiting a Ki value of 19.18 nM. This compound inhibits NECA-mediated cAMP production with an IC50 of 0.089 μM and mitigates immunosuppressive effects by promoting IL-2 and IFN-γ secretion. Additionally, adenosine receptor antagonist 6 counteracts the immunosuppressive actions of adenosine on T-cell activation and cytokine release, demonstrating potential in inhibiting tumor growth in CT26/MC38 xenograft models. It is suitable for research focused on colon cancer. -
PAF Antagonist
Dersalazine sodium is a platelet-activating factor (PAF) antagonist that demonstrates significant anti-inflammatory properties in intestinal models. It has been shown to effectively downregulate IL-17 expression in rodent colitis studies, making it a valuable tool for investigating inflammatory bowel disease and related conditions. Its mechanism of action allows for exploration of PAF-related pathways in various biological contexts. -
PTP4A3 Inhibitor
JMS-053 is a potent and reversible inhibitor of PTP4A3, with an IC50 value of 18 nM. This compound also exhibits significant inhibitory activity against PTP4A1 and PTP4A2, with IC50s of 50 nM and 53 nM, respectively. Additionally, JMS-053 demonstrates inhibition of CDC25B and DUSP3 with IC50 values of 92.6 nM and 207.6 nM, respectively. Through mechanisms such as interference with RhoA and STAT3/p38 signaling pathways, JMS-053 effectively suppresses tumor cell proliferation and migration, making it a valuable tool for investigating various cancers, including ovarian, breast, and colon cancer.
