Catalog No.
Product Name
Application
Product Information
Citations
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Adenosine A3 Receptor Modulator
VUF8507 is an allosteric modulator of the adenosine A3 receptor, demonstrating a binding affinity with a Ki of 204 nM. This compound enhances A3 receptor activity and has potential applications in the study of inflammatory diseases and neuroprotection. Researchers may utilize VUF8507 to gain insights into the modulation of adenosine signaling pathways and their implications in various biological processes. -
Adenosine Receptor Agonist
2-Chloro-3-deazaadenosine is an adenosine receptor agonist that demonstrates specific interactions with A1, A2A, A2B, and A3 receptors, exhibiting inhibitory constants (Kis) of 0.3, 0.08, 25.5, and 1.9 μM, respectively. This compound is valuable in the study of adenosine signaling pathways and its diverse biological effects, making it suitable for research applications involving receptor pharmacology and cell signaling. -
A2A Adenosine Receptor Antagonist
MSX-2 is a potent antagonist of the A2A adenosine receptor, exhibiting a Ki of 5 nM in human tissues. This compound plays a significant role in the modulation of physiological processes associated with Parkinson's disease. MSX-2 can be utilized in research aimed at understanding the therapeutic effects of A2A receptor inhibition in neurological disorders. -
Adenosine Receptor Inhibitor
CVT-2759 is a potent inhibitor of the A1 adenosine receptor, exhibiting IC50 values of 0.18 μM and 9.5 μM to antagonize [3H]CPX binding in the absence and presence of 1 mM GTP, respectively. This compound is essential for assessing the modulation of AV nodal conduction, facilitating a reduction in ventricular rate without inducing AV block, bradycardia, atrial arrhythmias, or vasodilation. It serves as a valuable reagent for research on cardiovascular physiology and pharmacological modulation of adenosine receptor pathways. -
A1 Adenosine Receptor Antagonist
(Rac)-WRC-0571 is a potent and selective antagonist of A1 adenosine receptors, characterized by its non-xanthine structure and oral bioavailability. It effectively inhibits the binding of [3H]-N6-cyclohexyladenosine (CHA) to guinea pig A1 receptors, demonstrating a Ki value of 1.1 nM. This compound is valuable for research into adenosine receptor signaling and its implications in various physiological and pathological processes. -
Adenosine A3 Receptor Antagonist
KF26777 (free base) is a highly selective antagonist of the adenosine A3 receptor, exhibiting a Ki value of 0.2 nM. It demonstrates significant selectivity over adenosine A1, A2A, and A2B receptors, with factors of 9000-fold, 2350-fold, and 3100-fold, respectively. This compound effectively inhibits [125I]AB-MECA binding to adenosine A3 receptors and holds potential for research into brain ischemia and inflammatory diseases, such as asthma. -
A3AR Ligand
I-AB-MECA is a selective ligand for the A3 adenosine receptor (A3AR), functioning as an important tool in receptor binding studies. This radioligand is utilized in various biological research applications, including pharmacological profiling and understanding adenosine receptor signaling pathways. It aids in elucidating the role of A3AR in various physiological and pathological processes. -
A1AR Agonist
(±)-5'-Chloro-5'-deoxy-ENBA is an A1 adenosine receptor (A1AR) agonist that induces hypothermia in murine models. This compound is instrumental in studying the physiological effects and therapeutic potential of A1AR modulation. It serves as a valuable tool for researchers investigating adenosine signaling pathways and their implications in various biological processes. -
Adenosine Receptor Antagonist
Xanthine amine congener trihydrochloride is a potent antagonist of adenosine A1 and A2 receptors, exhibiting IC50 values of 1.8 nM and 114 nM, respectively. This compound is utilized in research applications focusing on the modulation of adenosine receptors and elucidating their roles in various physiological and pathological processes. Additionally, Xanthine amine congener has been characterized as a convulsant agent in murine models, aiding in the study of seizure mechanisms. -
A1AR Antagonist
L-97-1 is a selective antagonist of the A1 adenosine receptor (A1AR). This water-soluble small molecule exhibits high affinity for human A1AR, effectively blocking receptor activation. By competitively inhibiting A1AR, L-97-1 alleviates adenosine-induced bronchoconstriction and inflammation, making it a valuable tool in asthma research and the study of airway hyperreactivity. Its action can contribute to a better understanding of therapeutic approaches for respiratory conditions associated with adenosine signaling. -
Adenosine Receptor Agonist
LUF5831 is a selective adenosine A1 receptor agonist with a binding affinity of Ki = 18 nM. It exhibits pharmacological activity by modulating adenosine signaling pathways, making it valuable for research applications investigating neurological processes and cardiovascular functions. Its unique properties facilitate studies on adenosine receptor-mediated effects in various biological systems. -
Adenosine Receptor Antagonist
Dansyl-NECA is a dansyl-labeled antagonist of adenosine receptors, functioning primarily through the inhibition of adenosine signaling pathways. This compound serves as a valuable tool in studying the biological effects of adenosine receptor modulation, providing insights into cellular mechanisms involved in neuroprotection, inflammation, and cancer research. Its fluorescence properties enhance detection and visualization in biochemical assays. -
A2AAR Antagonist
A2AAR antagonist 1 is a selective antagonist of the adenosine A2A receptor (A2AAR) with a Ki value of 20 nM. This compound exhibits high ligand efficiency and is suitable for research into neurodegenerative diseases, offering potential insights into therapeutic strategies targeting A2AAR-related pathways. Its pharmacological properties make it a valuable tool for elucidating receptor functions and investigating the role of adenosine signaling in various biological contexts. -
A1 AdoR Partial Agonist
CVT-2759 analog is a partial agonist of the A1 adenosine receptor, exhibiting a Ki value of 167 nM. This compound is valuable for research into cardiac arrhythmias, providing insights into the modulation of adenosine receptor signaling and its implications in cardiac health. Its specificity for the A1 receptor makes it a suitable tool for studying the physiological effects of adenosine in cardiac tissue. -
A2A Antagonist
LUF5981 is a potent antagonist of the adenosine A2A receptor, exhibiting a pIC50 value of 6.7. This compound has shown efficacy in modulating adenosine receptor activity, making it a valuable tool for research in areas such as neuroprotection, immunology, and cancer therapy. Its application in preclinical studies can aid in the exploration of A2A-mediated pathways and their role in various biological processes. -
A2B AdoR Antagonist
CVT-5440 is a selective antagonist of the A2B adenosine receptor, exhibiting high affinity with a Ki value of 50 nM. It demonstrates significant selectivity over other adenosine receptor subtypes, including A1, A2A, and A3, with selectivity ratios greater than 200. This compound is suitable for research applications focusing on asthma and related respiratory conditions, where modulation of adenosine signaling is of interest. -
Adenosine A3 Receptor Antagonist
MRS1067 is a competitive antagonist of the adenosine A3 receptor, effectively inhibiting the suppression of adenylate cyclase induced by adenosine A3 receptor agonists and influencing G protein activation. This compound is valuable in research applications focused on inflammation and cancer, providing insights into the role of adenosine A3 receptor signaling in various physiological and pathological processes. -
A2B Adenosine Receptor Antagonist
PSB-1115 potassium salt is a selective antagonist of the A2B adenosine receptor, demonstrating significant inhibitory effects on the receptor's activity. This compound is particularly notable for its ability to block the contraction inhibition of acetylcholine induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS). It serves as a valuable tool for research into adenosine signaling pathways and the modulation of inflammation-related responses. -
Adenosine Receptor Binding Enhancer
PD81723 is an adenosine receptor binding enhancer that significantly boosts the inhibition of exogenous adenosine in a dose-dependent manner within hippocampal brain sections. This compound is vital for research exploring adenosine receptor modulation and its implications in neurological processes. Its ability to facilitate adenosine receptor interactions makes it an invaluable tool for studies focusing on cognitive function and related disorders. -
ADORA1 Modulator
ADORA1 modulator-1 is a selective modulator of the adenosine A1 receptor (ADORA1), known for its role in cellular signaling pathways. It demonstrates significant influence on neuroprotective and cardioprotective activities, making it valuable for the exploration of metabolic disorders and neurological diseases. This compound serves as a critical tool for researchers investigating the manipulation of adenosine receptor signaling in various biological contexts. -
A3AR Antagonist
A3AR Antagonist 5 is a selective antagonist of the human adenosine A3 receptor, demonstrating an affinity of pC 4.542 μM. This compound is valuable for research applications focused on investigating the role of A3 receptors in various physiological processes and pathological states. Its specificity may facilitate studies on adenosine-mediated signaling pathways and their implications in inflammation, cancer, and neuroprotection. -
A2AR Ligand
MNI-444 is a blood-brain barrier-permeable ligand for the adenosine A2A receptor (A2AR). This compound serves as a valuable tool in the investigation of non-dopaminergic pathways relevant to Parkinson's disease research. Its ability to selectively interact with A2AR positions it as a promising candidate for studying therapeutic strategies targeting neurodegenerative disorders. -
Adenosine A3 Antagonist
VUF8504 is a potent and selective antagonist of the adenosine A3 receptor, exhibiting a Ki value of 0.017 nM. This compound is primarily utilized in research focused on the modulation of adenosine signaling pathways, particularly in studies investigating the role of the A3 receptor in inflammation, neuroprotection, and cancer. Its high specificity makes VUF8504 a valuable tool for elucidating the biological functions of the A3 receptor in various physiological and pathological contexts. -
AdeR Agonist
N-(7H-Purin-6-yl)acetamide is a selective adenosine receptor (AdeR) agonist, exhibiting Ki values of 0.515 μM for the human adenosine receptor and 2.85 μM for the rat adenosine receptor. This compound has significant implications for research into adenosine receptor signaling pathways, pain mechanisms, inflammatory responses, and renal physiology. Its specificity for AdeR makes it a valuable tool for studying the role of adenosine in various biological processes. -
A2A Receptor Agonist
GW 328267 is an A2A receptor agonist that plays a pivotal role in modulating inflammatory responses. Its activation of the A2A receptor has potential applications in the study of asthma, chronic obstructive pulmonary disease (COPD), and upper respiratory inflammatory diseases. This compound serves as a valuable tool for researchers investigating the therapeutic implications of A2A receptor pathways in inflammatory conditions. -
Adenosine Receptor Antagonist
XCC is a 1,3,8-substituted xanthine derivative that functions as an adenosine receptor antagonist, exhibiting a Ki of 1.905 μM. This compound is valuable for studying adenosine receptor signaling pathways and their implications in various physiological processes and disease states. Research applications include pharmacological studies related to neuroprotection, inflammation, and cancer. -
Fluorinated Detergent
FLAC6 is a potent fluorinated detergent designed for the solubilization of membrane proteins, including the native adenosine receptor A2AR and two transporters, AcrB and BmrA. This reagent effectively preserves the structural and functional integrity of various membrane proteins, making it valuable for applications in structural biology and biophysical characterization. FLAC6 facilitates the study of GPCRs and transporters, enabling advancements in drug discovery and biochemical research. -
A2A Adenosine Receptor Agonist
2-Hexynyl-5′-N-ethylcarboxamidoadenosine is a selective agonist of the A2A adenosine receptor. It enhances intracellular cAMP levels and suppresses TNFα-induced MMP-3 release, indicating its anti-inflammatory potential. Furthermore, 2-Hexynyl-5′-N-ethylcarboxamidoadenosine promotes Aβ42 production in SH-SY5Y cells, making it a valuable tool for research on neurodegenerative diseases and receptor signaling pathways. -
Adenosine A2A Antagonist
ST4206 is a potent adenosine A2A receptor antagonist, exhibiting inhibitory constants (Kis) of 12 nM for the A2A receptor and 197 nM for the A1 receptor. This compound demonstrates significant biological activity, making it a valuable tool in the study of neurodegenerative disorders. ST4206 holds potential for advancing research in Parkinson's disease, providing insights into adenosine-mediated signaling pathways. -
Adenosine Receptor Antagonist
A2B receptor antagonist 1 is a selective antagonist of the A2B adenosine receptor. This compound demonstrates significant inhibition of adenosine-mediated signaling pathways, making it valuable in the investigation of adenosine receptor functions and their roles in various physiological and pathological conditions. A2B receptor antagonist 1 is applicable in research areas such as immunology, cancer biology, and neurobiology. -
Adenosine Receptor Antagonist
Sch412348 is a highly potent competitive antagonist of the human adenosine A2A receptor, exhibiting a Ki value of 0.6 nM and demonstrating over 1000-fold selectivity against other adenosine receptor subtypes. This selectivity makes Sch412348 a valuable tool for studying adenosine signaling pathways. It is particularly relevant in research focusing on neurological disorders, cardiovascular conditions, and cancer, where modulation of adenosine receptors may provide therapeutic insights. -
Adenosine Receptor Inhibitor
KF21213 is a selective adenosine A2A receptor inhibitor, demonstrating a high affinity with a Ki value of 3.0 nM. This compound is essential for research involving central nervous system (CNS) functions and disorders, providing valuable insights into adenosine receptor signaling pathways. Its precision in targeting A2A receptors makes it a suitable tool for studying their role in neuropharmacology and related therapeutic applications. -
Adenosine Receptor Agonist
UP202-56 is an adenosine receptor agonist that selectively activates adenosinergic signaling pathways. Its primary mechanism involves mimicking endogenous adenosine, leading to enhanced receptor-mediated cellular responses. This compound is essential for research applications focused on exploring adenosine-related physiological processes and the potential therapeutic implications in various diseases. -
Adenosine Receptor Antagonist
N-0861 racemate is a selective antagonist of the adenosine A1 receptor. It exhibits notable activity in modulating adenosine signaling pathways, making it valuable for research in neurology and cardiology. This compound is essential for investigating the physiological roles of adenosine receptors and their implications in various biological processes. -
A2B Receptor Antagonist
PSB-603 is a potent and highly selective antagonist of the A2B adenosine receptor, exhibiting a Ki value of 0.553 nM. This compound demonstrates minimal affinity for human and rat A1, A2A, and human A3 receptors at concentrations up to 10 μM. PSB-603 is primarily utilized in research exploring adenosine receptor signaling pathways and their implications in various physiological and pathological processes. -
Adenosine A3 Receptor Antagonist
MRS 1523 is a selective antagonist of the adenosine A3 receptor, demonstrating Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. It exhibits significant selectivity with 140-fold and 18-fold greater affinity for the A3 receptor over A1 and A2A receptors in rat models. MRS 1523 has been shown to produce an antihyperalgesic effect by blocking N-type calcium channels and inhibiting action potentials in isolated rat dorsal root ganglion (DRG) neurons, making it valuable for research in pain mechanisms and receptor activity. -
A2B Adenosine Receptor Antagonist
PSB-1115 is a selective antagonist of the A2B adenosine receptor, providing a valuable tool for investigating adenosine signaling pathways. It effectively inhibits the contraction induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS) in response to acetylcholine (ACh). This compound is relevant for research in inflammation, smooth muscle function, and potential therapeutic interventions targeting adenosine receptors. -
A3 Adenosine Receptor Antagonist
DPTN dihydrochloride is a potent and selective antagonist of the A3 adenosine receptor (A3AR), exhibiting Ki values of 1.65 nM for human, 9.61 nM for mouse, and 8.53 nM for rat receptors. This compound is valuable for research applications investigating the physiological roles of A3AR in various biological processes, including immunomodulation and tumor growth regulation. DPTN's selectivity makes it an important tool for studies aimed at elucidating the therapeutic potential of A3AR modulation in human and animal models. -
A3 Receptor Antagonist
MRS1220 is a highly potent and selective antagonist of the human A3 adenosine receptor (hA3AR), exhibiting a Ki value of 0.59 nM. This compound is of significant interest for research related to diseases of the central nervous system and has demonstrated the ability to reduce glioblastoma tumor size and inhibit angiogenesis in vivo. Its distinct action on the A3 receptor makes it a valuable tool for studying mechanisms associated with neuroprotection and tumor biology. -
GPCRs/Adenosine Modulator
SCH-202676 hydrobromide is an allosteric modulator targeting G protein-coupled receptors (GPCRs), specifically the adenosine receptor. This compound demonstrates notable antiviral activity and effectively inhibits the 3CLpro enzyme in a time-dependent manner, with an IC50 value of 0.655 μM. Its unique mechanism makes it a valuable reagent for research applications focused on GPCR modulation and antiviral studies. -
Adenosine Receptor Activator
Adenosine-2'-monophosphate (2'-AMP) functions primarily as an adenosine receptor activator. This compound is metabolized to extracellular adenosine through the extracellular 2’,3’-cAMP-adenosine pathway, playing a crucial role in modulating immune responses. Research indicates that 2'-AMP inhibits lipopolysaccharide (LPS)-induced production of TNF-α and CXCL10 via activation of the A2A receptor, making it a valuable tool in studies of inflammation and immune regulation. -
Adenosine Receptor Antagonist
7-Methylxanthine is a non-selective adenosine receptor antagonist that serves as an orally active methyl derivative of xanthine. This compound has demonstrated key biological activities, including anti-myopia effects, making it valuable for research in visual function and ocular health. Additionally, 7-Methylxanthine is a component of human urinary calculi, highlighting its relevance in studies related to purine metabolism and urolithiasis. -
A2A Receptor Antagonist
Inupadenant is a potent and selective antagonist of the A2A adenosine receptor, primarily utilized for its immunomodulatory effects. This compound enhances the humoral immune response and exhibits promising anti-tumor activity, making it a valuable tool in cancer research and immune response studies. Notably, Inupadenant does not penetrate the blood-brain barrier, which may limit its central nervous system effects. -
A2A Inverse Agonist
Sipagladenant is an orally active inverse agonist of the adenosine A2A receptor. It is primarily utilized in research related to frontal lobe dysfunction, offering insights into the modulation of adenosine signaling pathways. This compound may be useful in elucidating the role of A2A receptors in various neurological conditions. -
A1 Adenosine Receptor Antagonist
PSB36 is a selective antagonist of the A1 adenosine receptor, exhibiting a Ki of 0.12 nM and Kd of 0.7 nM. This compound has demonstrated efficacy in reducing formalin- and carrageenan-induced edema in murine models, alongside a decrease in pain-related behaviors without causing local paw effects. Furthermore, PSB36 prolongs the action potential duration (APD90) of rat and human atria, enhances frequency-dependent atrial effective refractory period (ERP), raises diastolic thresholds, and mitigates the duration of atrial fibrillation episodes. PSB36 is applicable in research investigating inflammatory pain, hyperalgesia, edema, and atrial fibrillation. -
Adenosine A2A Receptor Antagonist
(E)-8-(3-Chlorostyryl)caffeine is a selective antagonist of the adenosine A2A receptor, which plays a significant role in neuronal signaling. In addition to its primary action, this compound also inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM through a mechanism independent of its effects on the A2A receptor. Due to its dual activity, (E)-8-(3-Chlorostyryl)caffeine is of particular interest in research related to Parkinson's disease and other neurological disorders. -
A2AAR Agonist
UK-432097 is a highly potent and selective agonist of the A2A adenosine receptor (A2AAR), exhibiting a pKi of 8.4 for human A2AAR. This compound demonstrates significant anti-inflammatory and anti-aggregatory properties, making it a valuable tool for studying inflammatory pathways. UK-432097 is particularly relevant for research applications related to chronic obstructive pulmonary disease (COPD) and other conditions influenced by A2A receptor signaling. -
A2BAR Antagonist
ISAM-140 is a potent and selective antagonist of the A2B adenosine receptor, exhibiting a Ki of 3.49 nM. This compound is valuable for research applications focused on adenosine signaling pathways and their role in various physiological processes. Its high specificity makes it an essential tool for studying the therapeutic potential of A2B receptor modulation in disease models. -
Adenosine Receptor Agonist
(-)-N6-Phenylisopropyl adenosine is a selective agonist for the A1 adenosine receptor. This compound effectively inhibits K+-induced Ca2+ uptake with an IC50 of 0.5 µM. It has been shown to protect against ischemia-induced ventricular arrhythmias and atrial fibrillation, while also exacerbating symptoms associated with ethanol withdrawal. Additionally, (-)-N6-phenylisopropyl adenosine exhibits notable analgesic properties, making it a valuable tool for research in cardiovascular and pain-related studies. -
A3 Adenosine Receptor Antagonist
MRS-1191 is a selective antagonist of the A3 adenosine receptor, exhibiting a KB value of 92 nM and a Ki value of 31.4 nM for the human A3 receptor. This compound demonstrates an IC50 of 120 nM in CHO cells, making it an effective tool for investigating A3 receptor-related biological pathways. Additionally, MRS-1191 features an alkyne group, enabling its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.
