Catalog No.
Product Name
Application
Product Information
Citations
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NK3 receptor antagonist
Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. -
5HT1A antagonist
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT. -
5-HT/dopamine receptor antagonist
Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
LPA2 agonist
GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM). -
glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI). -
5-HT3 receptor antagonist
Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor. -
5HT3 receptor antagonist
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. -
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. - Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
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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.
