Catalog No.
Product Name
Application
Product Information
Citations
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A2AAR Antagonist
LJ-4517 is a highly selective antagonist of the adenosine A2A receptor (A2AAR) with a binding affinity (Ki) of 18.3 nM. This compound effectively displaces the binding of [3H]ZM241385 at wild-type A2AAR, demonstrating its potency in modulating adenosine signaling pathways. Additionally, LJ-4517 features an alkyne moiety, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) applications. This dual functionality makes it a valuable tool for diverse biochemical research. -
A2A/A1 AR Antagonist
A2A/A1 AR antagonist-1 is a dual-target antagonist for the A2A and A1 adenosine receptors, exhibiting binding affinities (Kis) of 5.58 nM and 24.2 nM, respectively. It serves as a valuable tool for research related to ischemic stroke, providing insights into receptor interactions and potential therapeutic pathways. This compound is suitable for studies exploring adenosine receptor modulation in various biological contexts. -
A3AR Antagonist
A3AR antagonist 3 is a selective antagonist of the A3 adenosine receptor, exhibiting a Ki value of 37 nM. It demonstrates over 60-fold selectivity against A1 and A2A adenosine receptors. This compound is useful for investigating the role of A3AR in various biological processes and therapeutic applications, including inflammation and cancer research. -
Adenosine Receptor Antagonist
Bamifylline is a xanthine derivative that selectively antagonizes the adenosine A1 receptor. This compound is known to exhibit biological activities related to the modulation of adenosine signaling pathways, making it valuable for research in cardiovascular and neuroprotective studies. Its role as an adenosine receptor antagonist facilitates investigations into cellular responses mediated by adenosine, contributing to the understanding of various physiological and pathological processes. -
A1-adenosine Antagonist
(6R)-Naxifylline is a selective A1-adenosine antagonist that exhibits notable saluretic activity. This compound demonstrates the ability to induce relaxation of spontaneous tone in guinea pig trachea, making it a valuable tool for studying adenosine receptor pathways. Its unique pharmacological profile supports research applications in respiratory physiology and cardiovascular studies. -
Adenosine A3 Receptor Agonist
CP-608039 is a selective agonist for the adenosine A3 receptor, demonstrating potency in targeting this specific receptor. It has significant biological activity in studies related to ischemic myocardial injury, making it a valuable tool for researchers investigating cardiac protection and therapeutic interventions in ischemic conditions. Its unique mechanism of action allows for detailed exploration of adenosine-mediated pathways in cardiovascular research. -
A3AR Agonist
A3AR agonist 4 is a selective agonist of the A3 adenosine receptor (A3AR), exhibiting a Ki value of 1.24 nM for human A3AR. This compound effectively inhibits cyclic AMP (cAMP) production with an EC50 of 0.17 nM. A3AR agonist 4 is valuable for investigating mechanisms of inflammation and pain modulation in various biological studies. -
A3AR Modulator
MRS8247 is a positive allosteric modulator of the A3 adenosine receptor (A3AR), enhancing the receptor's activity and stability. This compound has been shown to slow the dissociation rate of agonists, thereby prolonging their biological effects. MRS8247 is valuable for research applications focused on adenosine signaling and its implications in physiological and pathological processes. -
Adenosine Receptor Antagonist
Zaladenant is an adenosine receptor antagonist predominantly targeting the A2A receptor subtype. This compound exhibits notable antitumor activity, making it relevant for investigations into cancer biology and treatment strategies. Its ability to modulate adenosine signaling pathways provides a valuable tool for research focused on tumor microenvironments and immune response. -
adenosine A3 receptor Antagonist
LJ-2698 is an orally active antagonist of the adenosine A3 receptor. This compound demonstrates significant anti-inflammatory effects by increasing levels of anti-inflammatory cytokines and promoting the proliferation of M2 macrophages in lung tissues, leading to improved pulmonary function and reduced alveolar cavity enlargement. Additionally, LJ-2698 has shown potential in preventing renal injury associated with diabetic nephropathy by inhibiting lipid accumulation and enhancing PGC1α expression in renal tissues. This reagent is suitable for research applications related to emphysema and diabetic nephropathy. -
A3AR PAM
A3AR Modulator 1 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). This compound significantly enhances the Cl-IB-MECA-stimulated [35S]GTPγS binding Emax, indicating its capacity to potentiate receptor activity. It is a valuable tool for research applications involving adenosine signaling pathways and may aid in the exploration of therapeutic targets related to inflammation, cancer, and neurodegenerative diseases. -
Adenosine Receptor Antagonist
ATL444 is a selective adenosine receptor antagonist that exhibits Ki values of 7.0 nM for the rA1AR receptor, 2.5 nM for rA2AAR, 61.8 nM for rA2BAR, and >1000 nM for rA3AR. This compound is valuable for research applications focused on the modulation of adenosine signaling pathways, which are implicated in various physiological processes and disease states. ATL444 can aid in elucidating the role of adenosine receptors in pharmacological studies, offering insights into their potential as therapeutic targets. -
Adenosine A2A Antagonist Prodrug
Lu AA47070 is a phosphonooxymethylene prodrug designed to selectively antagonize the Adenosine A2A receptor. It effectively reverses the motor and motivational impairments induced by dopamine D2 receptor antagonists. This compound is of particular interest in research focused on neuropsychiatric disorders and the interplay between dopaminergic and adenosinergic systems. -
A1AR Antagonist
A1AR antagonist 2 is a potent antagonist of the A1 adenosine receptor (A1AR), exhibiting inhibitory constants (Kis) of 1.49 nM for hA1, 10.2 nM for hA2A, and 50.1 nM for hA2B. This compound is valuable for research applications focused on the modulation of adenosine signaling pathways and their effects on physiological and pathological processes. Its selective inhibition of A1AR makes it a useful tool in pharmacological studies involving cardiovascular, neurological, and metabolic research. -
A1-AR Ligand
DU172 is a potent ligand for the adenosine A1 receptor (A1AR), exhibiting an IC50 of 24.9 nM. It also shows an affinity for the A2A receptor (A2AAR) with an IC50 of 0.42 μM. This compound is valuable for studies involving adenosine receptor signaling and can aid in research related to cardiovascular, neuroprotective, and anti-inflammatory mechanisms. -
A2aR Antagonist
A2A receptor antagonist 3 is a potent adenosine A2A receptor antagonist with a Ki of 0.4 nM. This compound also exhibits binding affinity for A2B, A1, and A3 receptors, with Ki values of 37 nM, 107 nM, and 1467 nM, respectively. It is valuable for research applications involving adenosine signaling pathways and pharmacological studies related to various physiological processes and diseases. -
Adenosine Receptor Antagonist
Lu AA41063 is an antagonist of the adenosine A2A receptor, exhibiting a Ki value of 5.9 nM for the human A2A receptor. This compound demonstrates potential therapeutic effects in the treatment of Parkinson's disease by modulating adenosine signaling pathways. It is a valuable reagent for research focused on neurodegenerative disorders and the pharmacological exploration of adenosine receptors. -
A2AR Antagonist
A2AR-antagonist-1 is a selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 29 nM. This compound demonstrates significant anti-tumor activity and maintains metabolic stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, A2AR-antagonist-1 activates T cells by inhibiting immunosuppressive molecules such as LAG-3 and TIM-3, while promoting the expression of effector molecules including GZMB, IFNG, and IL-2, making it a valuable tool in cancer immunotherapy research. -
Adenosine Receptor Agonist
AMP-579 is an adenosine receptor agonist targeting the adenosine A1 and A2A receptors, exhibiting Ki values of 1.7 nM and 4.5 nM for A1 receptors in rat brain and adipocytes, and a Ki value of 56 nM for A2A receptors in rat brain. This compound effectively inhibits lipolysis and restores insulin-dependent glucose transport through A1 receptor activation, while it promotes vasodilation, especially in coronary arteries, via A2A receptor activation with an IC50 of 0.3 μM in porcine coronary arterial rings. AMP-579 holds potential in cardioprotection and the therapeutic management of acute myocardial infarction. -
Adenosine Receptor antagonist
1,9-Dimethylxanthine is an antagonist of adenosine receptors, effectively blocking adenosine's effects on the central nervous system. This compound enhances neuronal excitability through modulation of the adenosine signaling pathway. 1,9-Dimethylxanthine serves as a valuable pharmacological tool in research aimed at investigating physiological and pathological mechanisms associated with adenosine. -
A3AR Agonist
MRS5663 is a potent A3 adenosine receptor (A3AR) agonist, demonstrating an EC50 of 5.62 nM in β-arrestin2 recruitment assays. This compound exhibits significant cytoprotective effects, particularly in models of skeletal muscle ischemia-reperfusion injury and claudication. Its unique mechanism and biological activity make it a valuable tool for research in cardiovascular and metabolic disorders. -
Adenosine A2A Receptor Agonist
LASSBio-1359 is an agonist of the adenosine A2A receptor, known for its vasodilatory and anti-inflammatory properties. This compound has potential applications in cardiovascular research and the study of inflammatory diseases, making it a valuable tool in exploring adenosine receptor signaling pathways and their relevance to various physiological and pathological conditions. -
A3AR Agonist
A3AR Agonist 5 is a potent activator of the A3 adenosine receptor (A3AR), exhibiting EC50 and Ki values of 0.14 nM and 6.36 nM for cAMP and human A3 receptors, respectively. This compound is valuable for research into pain modulation and inflammation, making it a significant tool for studies examining adenosine receptor signaling pathways and their therapeutic implications. -
A2AR-D2R Heteromer Ligand
Heterobivalent ligand-1 is a potent heterobivalent ligand targeting the Adenosine A2A-dopamine D2 receptor heteromer, exhibiting binding affinities of 2.1 nM for A2AR and 0.13 nM for D2R. This compound is valuable for studying receptor heteromerization and signal transduction in neurological research. Its unique design enables exploration of the functional interplay between these receptors in various biological contexts. -
Adenosine A3 Receptor Antagonist
MRS1097 is a potent antagonist of the human adenosine A3 receptor, exhibiting a Ki value of 100 nM. This compound effectively inhibits A3 receptor activity, making it a valuable tool for investigating adenosine signaling pathways and their implications in various physiological and pathological processes. MRS1097 is suitable for research applications focused on inflammation, cancer, and neuroprotection. -
Adenosine Receptor Agonist
Neladenoson dalanate hydrochloride is an orally active adenosine A1 receptor agonist precursor. This compound demonstrates significant biological activity as a partial agonist, making it a valuable tool in research related to chronic heart diseases. Its favorable pharmacokinetic properties and safety profile enhance its potential for therapeutic applications in cardiology. -
A3AR Agonist
MRS 5980 is a potent A3 adenosine receptor (A3AR) agonist with a Ki value of 0.7 nM, demonstrating high specificity for this receptor subtype. This compound exhibits notable oral bioavailability, making it suitable for in vivo studies. MRS 5980 is employed in research to investigate the physiological roles of A3AR in various biological processes and potential therapeutic applications in inflammation and cancer. -
A2AR Antagonist
A2A receptor antagonist 2 is a highly selective antagonist of the adenosine A2A receptor (A2AR) with an IC50 of 8.3 nM. This compound exhibits significant inhibitory activity, making it valuable for research into the modulation of adenosine signaling pathways. Its application spans various fields, including neurobiology and immunology, particularly in studies focused on inflammation and neurodegenerative diseases. -
A2aR Modulator
A2AR modulator-1 is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR) with an IC50 value of 9 nM. This compound reduces the affinity of endogenous adenosine for A2aR and inhibits activation of the cAMP signaling pathway. A2AR modulator-1 effectively enhances pCREB phosphorylation in CD4+ T cells, counteracting immunosuppression in the tumor microenvironment. Its ability to suppress tumor growth and metastasis has been demonstrated in models of triple-negative breast cancer, highlighting its potential in cancer research. -
Adenosine Receptor Antagonist
MRS7799 is a selective antagonist of the A3 adenosine receptor, demonstrating high affinity with Kds of 0.55 nM for human, 3.74 nM for mouse, and 2.80 nM for rat A3AR. This compound is particularly valuable in research applications related to neurodegeneration, cancer, and ischemic conditions in the heart and brain, as well as autoimmune inflammatory diseases. MRS7799 allows for the exploration of adenosine signaling pathways and their implications in various pathological states. -
Vasodilator/A2A Adenosine Receptor Agonist
Regadenoson hydrate is a selective A2A adenosine receptor agonist and potent vasodilator. It enhances coronary blood flow, making it valuable for myocardial perfusion imaging studies. Additionally, regadenoson hydrate increases the permeability of the blood-brain barrier (BBB) in rodent models, facilitating research into the enhanced delivery of therapeutic agents to the central nervous system (CNS) in humans. -
A3AR Antagonist
A3AR Antagonist 1 is a highly selective antagonist of the human A3 adenosine receptor (A3AR), exhibiting a Ki of 4.63 nM. This compound demonstrates no affinity for the rat A3AR, even at elevated concentrations. It is suitable for research applications focusing on adenosine signaling pathways and their roles in various physiological and pathological processes. -
hA3AR Antagonist
A3AR antagonist 2 is a potent inhibitor of the human A3 adenosine receptor (hA3AR) with a Ki value of 4.54 nM. This compound functions through competitive blockade of receptor activity, making it a valuable tool for elucidating A3AR-mediated signaling pathways. It is suitable for research applications investigating the role of A3AR in various biological processes, including inflammation and cancer biology. -
Adenosine Receptor Agonist
Neladenoson dalanate is a selective agonist precursor of the Adenosine A1 Receptor. This compound exhibits notable pharmacokinetic properties and a favorable safety profile, making it suitable for research in chronic heart disease. Its biological activity contributes to the modulation of cardiac function, offering insights into potential therapeutic applications for cardiovascular disorders. -
A1-adenosine Agonist
SDZ-WAG994 is a selective and orally active agonist of the A1-adenosine receptor, exhibiting a KD of 23 nM. This compound is characterized by its stability and long action, making it suitable for research applications related to atrial fibrillation. Its specificity for the A1 receptor facilitates investigations into adenosine receptor signaling pathways and potential therapeutic interventions in cardiovascular diseases. -
Adenosine Receptor Agonist
MRS8028 is a selective agonist for the A3 adenosine receptor (A3AR), demonstrating a binding affinity with a Ki of 2.44 nM. This compound exhibits potential therapeutic effects in the modulation of ischemia and inflammatory diseases, making it a valuable tool for researchers investigating adenosine signaling pathways in pathological conditions. Its efficacy in targeting A3AR may provide insights into novel treatment approaches for related diseases. -
A₂B Adenosine Receptor Antagonist
SYAF080 is a selective antagonist of the human A₂B adenosine receptor (hA₂B AdoR), exhibiting a binding affinity with a Ki of 23.6 nM and a KB of 25.2 nM. This compound does not exhibit inhibition of human CYP450 cytochromes, making it suitable for pharmacological studies. SYAF080 is valuable for research focused on inflammation, metabolic disorders, and cardiovascular diseases, providing insights into the therapeutic potential of A₂B receptor modulation. -
A1AR Antagonist
A1AR Antagonist 1 is a selective antagonist of the A1 adenosine receptor, exhibiting Ki values of 2.08 nM for human A1, 6.91 nM for human A2A, and 31.2 nM for human A2B receptors. This compound demonstrates significant biological activity in modulating adenosine signaling pathways, making it valuable for research applications related to cardiovascular diseases, neuroprotection, and cancer progression. Its potency and selectivity provide a useful tool for studying the role of A1AR in various biological processes. -
A1-Adenosine Antagonist
Naxifylline is a potent and selective A1-adenosine antagonist, exhibiting Ki values of 0.67 nM for rat A1 receptors and 0.45 nM for cloned human A1 receptors. This compound serves as a potassium-sparing diuretic, making it useful for investigating edema related to congestive heart failure. Naxifylline's mechanism of action provides critical insights into adenosine receptor signaling and its implications in cardiovascular research. -
Hypnotic Agent
YGZ-331 is a hypnotic agent that primarily targets adenosine receptors A1R and A2aR. It enhances GABA levels and exerts a sedative-hypnotic effect by inhibiting the phosphorylation of CaMKII (pCaMKII). This compound has demonstrated the ability to reduce spontaneous motor activity in mice, making it a valuable tool for research into sedative mechanisms and sleep-related studies. -
A2A/A3 AR Antagonist
A2A/A3 AR antagonist-1 is a dual antagonist of the human A2A and A3 adenosine receptors, exhibiting dissociation constants (Kis) of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively. This compound serves as a fluorescent ligand, facilitating the study of adenosine receptor signaling pathways. Its biological activity makes it a valuable tool for research applications in pharmacology, receptor biology, and the development of therapies targeting adenosine-related disorders. -
Adenosine A1 Receptor Antagonist
NPC 200 is a potent and selective antagonist of the Adenosine A1 receptor. It effectively reverses NECA-induced left and right atrial depression, demonstrating EC50 values of 1.08 and 2.03 μM, respectively. This compound is valuable for research into cardiovascular function and the role of adenosine receptors in various physiological processes. -
Adenosine Receptor Agonist
Adenosine Receptor Agonist 2 is a potent adenosine A2B receptor (A2BR) agonist with an EC50 of 0.38 nM. This compound effectively inhibits the accumulation of cyclic AMP (cAMP) and calcium, demonstrating its role in modulating intracellular signaling pathways. Adenosine Receptor Agonist 2 is suitable for research applications focused on cardioprotection and related cardiovascular studies. -
A1/A3 Antagonist
A1/A3 AR antagonist 1 is a potent dual antagonist of the adenosine A1 and A3 receptors, exhibiting affinity constants (Kis) of 36.7 nM for human A1, 25.4 nM for human A3, and 1.47 nM for rat A1. This compound is valuable for investigating various biological processes, particularly in the context of kidney failure, inflammatory pulmonary diseases, and Alzheimer's disease. Its dual receptor targeting makes it a useful tool for exploring the roles of adenosine receptors in these conditions. -
Adenosine Receptor Antagonist
Xanthine amine congener dihydrochloride is a potent antagonist of adenosine A1 and A2 receptors, exhibiting IC50 values of 1.8 nM and 114 nM, respectively. This compound has demonstrated convulsant activity in murine models, making it a valuable tool for studying adenosine receptor involvement in neurological research and potential therapeutic applications. Its selectivity and potency make it suitable for investigations into the modulation of adenosine signaling and its implications in various physiological processes. -
A1 Adenosine Receptor Antagonist
IRFI-165 is a potent and selective antagonist of the A1 adenosine receptor, exhibiting a Ki value of 7.9 nM for the rat A1 adenosine receptor. This compound shows a high degree of selectivity over A2A and A3 receptors. IRFI-165 has demonstrated antidepressant activity in vivo, making it a valuable tool for studying psychiatric and neurological disorders in research applications. -
A1AR Antagonist
FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar affinity for this target. By effectively reducing interstitial adenosine levels, FSCPX can alter the impact of nucleoside transport inhibitors such as NBTI in cardiac tissue. This compound is valuable for research applications focused on cardiovascular pharmacology and adenosine signaling pathways. -
Adenosine Receptor Antagonist
Adenosine receptor antagonist 1 is a selective antagonist for the A2A adenosine receptor, exhibiting an IC50 of 0.29 nM. This compound demonstrates a 14-fold greater selectivity for A2A receptors compared to A2B receptors. It is widely used in research to investigate the modulatory effects of adenosine signaling in various physiological and pathological processes. -
Adenosine Receptor antagonist
N-0861 is a selective antagonist of the A1 adenosine receptor. It effectively inhibits the negative conduction effects associated with adenosine, such as prolonged AH interval and chest pain, without significantly affecting the increase in coronary blood flow velocity induced by adenosine. This specificity makes N-0861 a valuable tool for research in cardiovascular physiology and the exploration of adenosine receptor signaling pathways. -
Adenosine Analog
8-Methoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and possesses potential anti-cancer properties by inhibiting tumor progression. It is valuable for research applications in cardiovascular studies and cancer biology, providing insights into adenosine's role in these processes.
