Catalog No.
Product Name
Application
Product Information
Citations
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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. -
A2 Agonist
CI-936 is an orally active A2 adenosine receptor agonist exhibiting an affinity of 25 nM. This compound demonstrates significant and selective activities in preclinical models associated with antipsychotic efficacy. Notably, CI-936 effectively inhibits exploratory behavior in mice, making it a valuable tool for understanding the neuropharmacological pathways linked to psychotropic effects. -
Adenosine Receptor Antagonist
Swertisin is an adenosine A1 receptor antagonist with additional SGLT2 inhibitory activity. This compound exhibits various biological functions, including anti-diabetic and antioxidant properties, as well as the ability to inhibit hepatitis B virus (HBV). Research has demonstrated that Swertisin can enhance cognitive function and alleviate memory impairments in murine models, making it a valuable tool for studies in diabetes, neuroprotection, and viral infections. -
Drug Metabolite
1-epi-Regadenoson is an α-isomer impurity of Regadenoson, a potent and selective agonist for the adenosine A2A receptor. This compound is primarily used in research to investigate the pharmacological effects of adenosine receptor activation and its implications in cardiovascular function. The study of 1-epi-Regadenoson can aid in understanding the metabolic pathways and potential therapeutic effects associated with adenosine receptor modulation. -
Adenosine A2A Receptor Inhibitor
4-Desmethyl Istradefylline is a selective adenosine A2A receptor antagonist, serving as a significant metabolite of Istradefylline. With a Ki of 2.2 nM, it demonstrates potent inhibition of the A2A receptor, making it relevant for exploring therapeutic strategies in Parkinson's disease and related neurological disorders. Its oral bioactivity allows for convenience in in vivo research applications targeting adenosine signaling pathways. -
Drug Intermediate
1-epi-Regadenoson ethyl ester is a key intermediate in the synthesis of the α-isomer impurity of Regadenoson, a highly selective agonist for the adenosine A2A receptor. This compound is essential for research involving adenosine receptor biology and contributes to the understanding of cardiovascular function and cellular signaling pathways. Its application extends to the development and analysis of therapeutic agents targeting adenosine receptors. -
Drug Intermediate
1-epi-Regadenoson hydrazone serves as a crucial intermediate in the synthesis of the α-isomer impurity of Regadenoson, a selective adenosine A2A receptor agonist. Its role in the development of this compound is significant for research in cardiovascular pharmacology and adenosine receptor modulation. This reagent is essential for investigations into therapeutic applications targeting the A2A receptor pathway. -
Drug Intermediate
2,6-Dichloropurine is a pharmaceutical intermediate primarily utilized in the synthesis of various drug candidates. This compound plays a key role in the development of phosphodiesterase (PDE) inhibitors, human A3 adenosine receptor antagonists, and cyclin-dependent kinase (CDK) inhibitors. Its versatile chemical structure makes it a valuable reagent in biomedical research and pharmaceutical development. -
Drug Derivative
Benzoadenosine is a drug derivative that acts as an adenosine receptor modulator. It exhibits biological activities that may influence cellular signaling pathways involving adenosine, making it valuable for research in pharmacology and drug development. This compound can be utilized to investigate the role of adenosine-related mechanisms in various biological processes and disease states. -
Drug Derivative
MRS 2500 is a potent drug derivative that selectively targets adenosine A3 receptors. This compound exhibits significant effects on cellular signaling pathways, making it valuable for research involving inflammation and cancer biology. MRS 2500 can be utilized in studies aimed at understanding the role of adenosine receptors in various physiological and pathological processes. -
Alkaloid
N-(2-Hydroxy-3-methylbutyl)-adenosine is a natural alkaloid that modulates adenosine receptors. Its biological activity includes influencing various cellular processes such as inflammation and neuroprotection. This compound is utilized in research exploring adenosine signaling pathways and its implications in physiological and pathological conditions. -
Endogenous Metabolite
8-(3-Chlorostyryl)caffeine is a selective antagonist of the A2a adenosine receptor, demonstrating a significant 520-fold selectivity in radioligand binding assays conducted in rat brain. It effectively inhibits adenylylase with a 22-fold selectivity in rat chromaffin cells. Co-administration with the A1-selective antagonist CPX has been shown to enhance exercise activity. Additionally, 8-(3-Chlorostyryl)caffeine exhibits potent inhibitory activity against MAO-B in primate mitochondrial systems. This compound serves as a valuable tool for studying adenosine receptor signaling and its effects on physiological processes. -
Natural Product
4-(cis)-Acetyl-3,6,8-trihydroxy-3-methyldihydronaphthalenone is a natural product derived from Senna siamea, primarily investigated for its interactions with adenosine receptors. Although it demonstrates very low affinity for the adenosine A1 receptor (Ki > 50 μM), its unique structural features may offer insights into the modulation of bioactive compounds in various biological systems. This compound can serve as a valuable tool in research exploring the pharmacological properties of natural products. -
A1AR Ligand
2-Thioadenosine is a selective ligand for the A1 adenosine receptor (A1AR), exhibiting a Ki value of 80.3 nM. This compound demonstrates minimal affinity for the A2A, A2B, and A3 adenosine receptor subtypes. Additionally, 2-Thioadenosine serves as a precursor for the synthesis of fluorescent agonists that selectively target the A3 adenosine receptor, making it valuable for research in pharmacology and receptor biology. -
β-Glucuronidase Inhibitor
β-Glucuronidase-IN-5 is a selective inhibitor of β-glucuronidase with an IC50 value of 39.8 μM. This compound demonstrates low cytotoxicity in PC-3 cells, with an IC50 greater than 30 μM, and shows no affinity for adenosine receptors A₁ and A₂A. β-Glucuronidase-IN-5 is useful for investigating diseases associated with overexpression of β-glucuronidase, including colon cancer, arthritis, and complications related to AIDS. -
Biochemical Assay Reagent
CGS 21680 sodium is an adenosine A2A receptor agonist that selectively activates the A2A receptor, influencing various signaling pathways. This compound exhibits biological activities such as modulation of neurotransmission and anti-inflammatory effects, making it useful in research involving neurological and cardiovascular studies. It is commonly employed in biochemical assays to explore the roles of adenosine receptors in cellular processes and their potential therapeutic applications. -
Biochemical Assay Reagent
1,3-Dipropyl-7-methylxanthine is a selective antagonist of adenosine receptors, primarily targeting the A1 subtype. It exhibits potent inhibitory effects on adenosine-mediated signaling pathways, making it valuable in biochemical assays for studying adenosine receptor functions. This compound is commonly utilized in research examining cellular processes influenced by adenosine, such as neurotransmission, inflammation, and metabolic regulation. -
Biochemical Assay Reagent
5'-Ethylcarboxamido-2',3'-isopropylidene adenosine is a selective agonist targeting A2B adenosine receptors. This compound enhances A2B receptor activity, making it valuable for investigating the physiological roles of adenosine signaling in various biological processes. It serves as a pertinent tool in biochemical assays and research applications aimed at understanding adenosine's effects and its potential as a therapeutic target in drug development. -
Biochemical Reagent
Nestifylline is a biochemical reagent that functions primarily as an antagonist of adenosine receptors. It exhibits significant activity in modulating airway constriction, making it a valuable tool for studying respiratory diseases, particularly bronchospasm. Researchers can utilize Nestifylline to explore mechanisms underlying airway responsiveness and potential therapies for respiratory disorders. -
Adenosine A1 Receptor Agonist
Adenosine 5'-monophosphate monohydrate is an adenosine A1 receptor agonist that plays a crucial role in cellular signaling pathways. This compound exhibits significant antiviral activity against Herpes Simplex Virus types 1 and 2 (HSV-1 and HSV-2), making it valuable for studies related to viral infections. Its modulation of adenosine receptors also provides insights into various physiological and pathological processes, offering applications in pharmacological research.

