Catalog No.
Product Name
Application
Product Information
Citations
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Adenosine Receptor Antagonist
Xanthine amine congener hydrochloride is a non-selective adenosine receptor antagonist. It exhibits significant biological activity, inducing convulsions in murine models, which may be useful for studying the role of adenosine receptors in neurological disorders. This reagent serves as a valuable tool for researchers investigating adenosine receptor signaling pathways and their implications in various physiological and pathological conditions. -
Adenosine Receptors Antagonist
9-Ethyladenine acts as a competitive antagonist of adenosine receptors, specifically targeting A1, A2A, and A3 subtypes. This compound demonstrates high affinity for these receptors, with Ki values of 27 nM, 46 nM, and 86 nM respectively. Importantly, 9-Ethyladenine exhibits no significant inhibitory effect on adenine phosphoribosyltransferase (APRT), making it suitable for studies involving adenosine receptor-related disorders, including nervous system diseases. Researchers can utilize this compound to further investigate the roles of adenosine receptors in various biological contexts. -
Adenosine Receptor Antagonist
VUF-5574 is a selective antagonist of the adenosine A3 receptor, exhibiting a Ki value of 4.03 nM for the recombinant human receptor. This compound is beneficial for studies investigating adenosine signaling pathways and their implications in various physiological processes. Its use as an antagonist makes it a valuable tool for elucidating the role of adenosine receptors in disease models and therapeutic research. -
Adenosine Receptor Antagonist
MRS-3777 hemioxalate is a selective antagonist of the adenosine A3 receptor, known for its role in various physiological processes. This compound inhibits adenosine signaling, making it a valuable tool for investigating the functions of adenosine receptors in cellular systems. It has potential applications in researching inflammatory responses, cancer biology, and cardiovascular diseases. -
A1AdoR Partial Agonist
GS-9667 is a selective partial agonist of the A1 adenosine receptor (A1AdoR). This N6-5'-substituted adenosine analog effectively reduces cyclic AMP levels and inhibits the release of nonesterified fatty acids from epididymal adipocytes, demonstrating IC50 values of 6 nM and 44 nM, respectively. Its ability to inhibit lipolysis suggests potential applications in research related to Type 2 diabetes (T2DM) and dyslipidemia by lowering free fatty acids (FFA). -
A1AR Agonist
2-Chloro-N-cyclopentyl-2′-C-methyladenosine is a potent and selective agonist for A1 adenosine receptors (A1AR). This compound effectively inhibits cAMP modulation in medium spiny neurons, specifically in both direct pathway (dMSNs) and indirect pathway (iMSNs) neuronal populations. Its role as an A1AR agonist makes it valuable for research into neuropharmacology and the modulation of synaptic transmission. -
A2A Adenosine Receptor Agonist
Evodenoson is a selective agonist of the A2A adenosine receptor, known for its potent anti-inflammatory properties. It demonstrates significant efficacy in mitigating inflammatory responses, decreasing intestinal fluid secretion, and reducing tissue damage and neutrophil infiltration in models of Clostridium difficile toxin A exposure. Evodenoson's protective effects are attributed to its ability to inhibit myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, as well as to decrease the production of tumor necrosis factor-alpha (TNF-α). This compound has valuable applications in studying inflammation-related disorders and potential therapeutic interventions. -
A2a Receptor Agonist
Apadenoson is an adenosine analog that selectively activates the adenosine A2a receptor, resulting in significant coronary vasodilation. This compound is primarily utilized in research focused on cardiovascular physiology and pathology, particularly in studies assessing the regulatory role of adenosine in vascular functions. Its specific receptor targeting makes it a valuable tool for investigating therapeutic strategies in ischemic heart conditions. -
α1A-Adrenergic Receptor Agonist
Cirazoline hydrochloride is a potent full agonist of the α1A-adrenergic receptor, exhibiting a competitive inhibition constant (Ki) of 120 nM. It also acts as a partial agonist at the α1B-adrenergic receptor with a Ki of 960 nM and the α1D-adrenergic receptor with a Ki of 660 nM. This compound is valuable for research applications involving α1-adrenergic signaling pathways and the study of cardiovascular and neurological conditions. -
A2 Receptor Agonist
CV1808, or 2-Phenylaminoadenosine, functions primarily as a non-selective agonist of the A2 adenosine receptors. It exhibits inhibitory constants (Kis) of 76 nM and 1450 nM for the A2A and A3 receptor subtypes, respectively. This compound is valuable in research applications focused on adenosine signaling pathways and the study of cardiovascular and neurological disorders. Its ability to modulate A2 receptor activity makes it a useful tool for understanding the physiological roles of adenosine in various biological systems. -
A2A Adenosine Receptor Agonist
Binodenoson is a potent and selective A2A adenosine receptor agonist with a KD of 270 nM. It serves as a short-acting coronary vasodilator, enhancing myocardial stress imaging when used in conjunction with radiotracers. Its ability to modulate cardiovascular responses makes it a valuable tool for research in cardiac function and imaging techniques. -
Adenosine Receptor Antagonist
M1069 is a selective, orally active dual antagonist of the A2A and A2B adenosine receptors, demonstrating over 100-fold selectivity against the A1 and A3 receptors. This compound effectively counteracts the immune-suppressive mechanisms mediated by adenosine, making it valuable in cancer research. Additionally, M1069 shows promise for anti-tumor activity, supporting its potential use in therapeutic strategies aimed at enhancing immune responses in tumor microenvironments. -
A2A Adenosine Receptor Antagonist
TC-G 1004 is an orally active antagonist of the A2A adenosine receptor, demonstrating high selectivity with Ki values of 0.44 nM for the human A2A receptor and 80 nM for the human A1 receptor. This compound is valuable in research applications targeting adenosine receptor signaling pathways, particularly in studies related to neurological disorders and cancer. Its efficacy as a selective A2A antagonist makes it a key tool for investigating the role of adenosine receptors in various biological processes. -
Adenosine Receptor Modulator
GP531 is a selective adenosine receptor modulator that enhances the localized levels of endogenous adenosine during ischemic conditions while remaining pharmacologically inert under basal state. This compound plays a crucial role in modulating adenosine signaling pathways, making it valuable for research applications related to ischemia, cellular metabolism, and cardiovascular studies. GP531 can be utilized to investigate therapeutic strategies targeting adenosine receptors in various disease models. -
AR Inhibitor
Adenosine receptor inhibitor 2 (compound 14b) is a selective antagonist of adenosine receptors, primarily targeting A1 and A2A subtypes. This compound exhibits a higher affinity for A1AR, with a Ki value of 52.2 nM, compared to 167 nM for A2AAR. Its potent inhibitory effects make it valuable for research exploring adenosine signaling pathways, and its applications may extend to studies in cardiovascular disease, cancer, and neurobiology. -
Adenosine A3 Receptor Antagonist
MRS1334 is a potent and selective antagonist of the human adenosine A3 receptor, exhibiting a Ki of 2.69 nM. This compound effectively disrupts the cardioprotective effects of Cl-IB-MECA, resulting in significant bradycardia and elevated ST segment changes. Additionally, MRS1334 features an alkyne group that enables its use in click chemistry, specifically facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This property positions MRS1334 as a valuable tool in chemical biology and therapeutic research. -
Adenosine Receptors Inhibitor
8-Chloro caffeine is an adenosine receptor inhibitor that binds with a Ki of 30 µM. This compound is known to potentiate UV-induced chromosomal aberrations in Cl-I Chinese hamster embryonic lung cells, making it relevant for studies in genotoxicity. As a derivative of the methylxanthine alkaloid caffeine, 8-Chloro caffeine serves as a useful tool for investigating the role of adenosine receptors in cellular responses and stress mechanisms. -
A2bR/A2aR Agonist
LUF5834 is a selective partial agonist of the A2B adenosine receptor (A2BR), with an EC50 of 12 nM. Additionally, LUF5834 exhibits partial agonistic activity at the A1 and A2A adenosine receptors, with Ki values of 2.6 nM and 28 nM, respectively. This compound is valuable in studies investigating adenosine signaling pathways, receptor pharmacology, and potential therapeutic applications related to the modulation of adenosine receptor activity. -
A2BAR Antagonist
PSB-1901 is a potent antagonist of the A2B adenosine receptor (A2BAR), exhibiting inhibition constants (Kis) of 0.0835 nM for human and 0.131 nM for mouse A2BARs. This compound is instrumental in the investigation of adenosine signaling pathways and their implications in cancer research. Its high selectivity and potency make it a valuable tool for elucidating the role of A2BAR in tumor biology and developing potential therapeutic strategies. -
Stable Isotope
Theobromine-d3 is a deuterium-labeled derivative of Theobromine, a methylxanthine naturally occurring in cacao beans. This stable isotope serves as a valuable tool for studying adenosine receptor A1 (AR1) signaling inhibition in research applications. Theobromine-d3 is essential for metabolic tracing, pharmacokinetic studies, and the exploration of purinergic signaling pathways. -
A2A Agonist
MRE 0094 (Sonedenoson) is a selective agonist of the adenosine A2A receptor, exhibiting a Ki value of 490 nM. This compound demonstrates significant anti-platelet and anti-inflammatory activities, making it valuable for research in cardiovascular and inflammatory disease studies. MRE 0094 is useful for investigating the therapeutic potential of targeting the A2A receptor in various biological contexts. -
A2B Receptor Antagonist
A2B receptor antagonist 2 is a selective antagonist of the adenosine A2B receptor, demonstrating Ki values of 2.30 μM for rat A1, 6.8 μM for rat A2A, and 3.44 μM for human A2B receptors. This compound is valuable for investigating the role of adenosine receptors in various biological processes and has potential applications in research related to inflammation, cancer, and cardiovascular diseases. -
A2a/A2b Adenosine Receptor Antagonist
Adenosine receptor antagonist 2 is a potent oral antagonist of the A2a and A2b adenosine receptors, exhibiting IC50 values of 1 nM and 3 nM, respectively. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. Its ability to block adenosine receptor signaling may provide insights into therapeutic strategies for malignancies influenced by the tumor microenvironment. -
Stable Isotope
Istradefylline-13C,d3 is a stable isotope-labeled version of Istradefylline, a highly potent and selective antagonist of the adenosine A2A receptor. With a Ki value of 2.2 nM, it demonstrates significant efficacy in experimental models of Parkinson's disease. This reagent is essential for studies involving receptor binding and pharmacokinetics, providing insights into the role of adenosine receptors in neurological disorders. -
A2A Receptor Antagonist
JNJ-40255293 is a selective antagonist of the human A2A receptor, exhibiting a high affinity with a Ki of 7.5 nM. This compound is primarily utilized in research related to neurodegenerative diseases, including Parkinson's disease, allowing for valuable insights into receptor signaling and potential therapeutic strategies. Its use as a research tool can aid in understanding the role of A2A receptors in various neurological conditions. -
Adenosine A3 Receptor Agonist
HEMADO is a selective adenosine A3 receptor agonist, demonstrating a high affinity with a Ki value of 1.1 nM for the human A3 subtype. This compound functions as a valuable tool in studying adenosine signaling pathways and related biological processes. Additionally, HEMADO features an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile reagent for click chemistry applications in chemical biology. -
A1AR Antagonist
A1AR Antagonist 6 is a potent and selective antagonist of the A1 adenosine receptor (A1AR), exhibiting a pIC50 of 6.38 and a pKi of 7.13. This compound effectively inhibits A1AR-mediated signaling pathways, making it a valuable tool for studying adenosine receptor physiology. Its specificity and potency enable its use in various research applications related to cardiovascular, neuroprotective, and inflammatory processes. -
A2B AR Positive Alosteric Modulator
KI-7 is a positive allosteric modulator of the A2B adenosine receptor. It enhances cAMP accumulation induced by the non-selective A2B agonist NECA, with an EC50 of 445.8 nM, and also increases cAMP levels in response to the selective agonist BAY 60-6583 and adenosine, exhibiting EC50 values of 2390 nM and 2550 nM, respectively. This compound is valuable for research in adenosine receptor signaling and modulation of associated pathways. -
Adenosine A1 Receptor Antagonist
Adenosine receptor antagonist 4 is a selective antagonist of the human adenosine A1 receptor, exhibiting a Ki value of 101 nM. This compound is valuable for studies investigating the role of adenosine signaling in physiological and pathological processes. It serves as a useful tool in pharmacological research related to cardiovascular, neuroprotective, and metabolic disorders. -
Adenosine Receptor Antagonist
KFM19 is a potent selective antagonist of the adenosine A1 receptor, exhibiting an IC50 of 50 nM. This compound has been demonstrated to inhibit A1 receptor activity, making it a valuable tool for studying adenosine signaling pathways. Its application in research includes the investigation of cardiovascular responses and the modulation of neuronal excitability, providing insights into potential therapeutic interventions for related disorders. -
A2A Receptor Agonist
PSB 0777 ammonium is a selective agonist of the adenosine A2A receptor, demonstrating a Ki of 44.4 nM for the rat A2A receptor and 360 nM for the human A2A receptor. It shows significantly reduced affinity for the A1 receptor, with Ki values exceeding 10,000 nM for rats and 541 nM for humans. While PSB 0777 ammonium exhibits limited brain penetration and is not orally absorbable, it holds potential for research applications in inflammatory bowel disease (IBS). -
Adenosine Receptor Antagonist
Adenosine receptor antagonist 3 is a selective antagonist of adenosine receptors, primarily targeting the A2A and A2B subtypes. This compound demonstrates significant potential in cancer research by modulating the adenosine signaling pathway, which plays a critical role in tumor immune evasion and progression. It may be utilized in studies to explore therapeutic strategies aimed at enhancing anti-tumor immunity. -
A2A Receptor Antagonist
Inupadenant hydrochloride is a selective antagonist of the A2A receptor, known for its oral bioactivity. This compound is unable to cross the blood-brain barrier, making it suitable for peripherally-targeted research applications. Inupadenant hydrochloride has been shown to enhance humoral immune responses and demonstrates anti-tumor activity, providing potential for investigations in immunotherapy and cancer treatment. -
Cardiotonic Agent
Sulmazole acts as a cardiotonic agent primarily through competitive inhibition of the A1 adenosine receptor. This mechanism enhances cardiac index while effectively reducing pulmonary capillary wedge pressure. Sulmazole is utilized in research focused on cardiovascular function and the modulation of cardiac output, making it relevant for studies aiming to improve cardiac performance in pathological conditions. -
A2A Adenosine Receptor Antagonist
DMPX (3,7-Dimethyl-1-propargylxanthine) serves as a selective antagonist of the A2A adenosine receptor, demonstrating a Ki of 11 μM for the rat A2 adenosine receptor and 45 μM for the rat A1 adenosine receptor. This compound effectively crosses the blood-brain barrier and protects dopaminergic and GABAergic neurons from mitochondrial dysfunction by inhibiting A2A receptor activity in specific brain regions. DMPX is pertinent for research into neurodegenerative disorders such as depression, Parkinson's disease, and Huntington's disease. -
A2AAR/hMAO-B Inhibitor
A2AAR/hMAO-B-IN-1 is a non-xanthine dual-target inhibitor that selectively inhibits the A2A adenosine receptor (A2AAR) with an IC50 of 34.9 nM, and human monoamine oxidase B (MAO-B) with a Ki of 39.5 nM. The compound effectively disrupts A2AAR-mediated cAMP accumulation and demonstrates competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 is suitable for research applications in neurodegenerative diseases, particularly in the study of Parkinson's disease (PD). -
Adenosine A2A Antagonist
MSX3 is a potent antagonist of the adenosine A2A receptor, demonstrating significant activity in modulating neuropharmacological responses. This compound has shown efficacy in reversing the effects of dopamine antagonism, specifically counteracting the impacts of Haloperidol on effort-related decision-making tasks in T-maze cost/benefit assessments. MSX3 is valuable for research exploring the roles of adenosine signaling in neurological disorders and the interplay between dopaminergic and adenosinergic systems. -
A2 AR Agonist
YT 146 is a potent agonist of the A2 adenosine receptor (A2 AR). It induces concentration-dependent accumulation of cyclic AMP, with an EC50 value of 1.5 nM. This compound exhibits cardioprotective effects, making it valuable for research into cardiovascular health and related therapeutic applications. -
A3AR Allosteric Enhancer
LUF6096 is a potent allosteric enhancer of the adenosine A3 receptor (A3AR), capable of enhancing agonist binding without exhibiting significant orthosteric affinity for any adenosine receptors. This compound demonstrates protective effects in myocardial ischemia/reperfusion injury, making it valuable for research in cardiovascular therapeutics and receptor biology. Its unique mechanism offers an innovative approach to modulating A3AR activity in related studies. -
Adenosine Receptor Antagonist
M1069 free base is a selective and orally active dual antagonist of the A2A and A2B adenosine receptors, demonstrating over 100-fold selectivity against A1 and A3 receptors. This compound counteracts the immune-suppressive effects of adenosine, making it valuable for research applications focused on cancer immunotherapy and potential anti-tumor activity. M1069's mechanism can inform studies aimed at understanding adenosine signaling pathways and their role in tumor microenvironments. -
A3AR Antagonist
A3AR Antagonist 4 is a potent antagonist of the A3 adenosine receptor, exhibiting Ki values of 30.8 nM for the human A3 receptor and 203 nM for the human A1 receptor. This compound is primarily utilized in research focused on cerebral ischemia, enabling investigations into its role in neuroprotection and inflammatory pathways associated with this condition. Through its selective blockade, A3AR Antagonist 4 serves as an important tool for elucidating the therapeutic potential of adenosine receptor modulation in neurological studies. -
Stable Isotope
Theobromine-d6 is a deuterium-labeled derivative of theobromine, a methylxanthine compound primarily found in cacao beans. This isotopically enriched reagent can be utilized in studies focusing on adenosine receptor A1 (AR1) signaling inhibition. It is suitable for quantitative analysis in metabolic studies and the investigation of the pharmacokinetics of theobromine and related compounds. -
Adenosine Receptor antagonist
A1/A3 AR antagonist 2 is an antagonist of the adenosine A1 and A3 receptors. This compound exhibits significant potential in studying neurological inflammatory diseases by modulating adenosine signaling pathways. Its application in research may enhance the understanding of the pathophysiology of various neurological disorders and the development of targeted therapies. -
A1AR Allosteric Modulator
TRR469 is a positive allosteric modulator of the A1 adenosine receptor (A1AR). It enhances the binding affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A1AR, thereby increasing the recognition of receptors by the agonist radioligand [³H]-CCPA. TRR469 demonstrates significant efficacy in preclinical models of anxiety and pain, making it a valuable tool for investigating anxiety disorders and developing pain management strategies. -
Adenosine Receptor Antagonist
Bamifylline hydrochloride is a xanthine derivative that functions as a selective antagonist of the adenosine A1 receptor. This compound exhibits significant biological activity in modulating adenosine signaling pathways, which may impact various physiological processes. Bamifylline hydrochloride is primarily utilized in research to explore its potential therapeutic effects on cardiovascular and respiratory disorders. -
A1AR Antagonist
A1AR antagonist 5 is a potent and selective antagonist of the A1 adenosine receptor (A1AR), exhibiting a pIC50 of 5.83 and a pKi of 6.11. This compound is valuable for research applications focused on the modulation of adenosine signaling pathways, cardiovascular protection, and neuroprotection. Its specificity makes it an ideal tool for investigating the therapeutic potential of A1AR antagonism in various disease models. -
A1R/A3R Dual Antagonist
A1/A3 AR Antagonist 3 is a dual antagonist targeting A1 and A3 adenosine receptors, exhibiting high affinity in the low-micromolar to low-nanomolar range. This compound is instrumental in researching chronic heart diseases, facilitating the exploration of mechanisms involved in cardiac function and pathology. Its selective inhibition of A1 and A3 receptors may provide insights into potential therapeutic strategies for related cardiovascular disorders. -
A3AR Agonist
MRS3558 is a potent and selective agonist of the A3 adenosine receptor (A3AR), exhibiting Ki values of 0.6 nM for human receptors and 0.9 nM for rat receptors. This compound is valuable for investigating the role of A3AR in neuropathic pain pathways and anesthetic responses. Its high selectivity and potency make it an essential tool for research in receptor pharmacology and therapeutic development. -
A2A Adenosine Antagonist
ST 1535 is a potent, orally active antagonist of the A2A adenosine receptor. It exhibits significant antiparkinsonian activity as well as antitremorigenic effects, making it a valuable tool for research on Parkinson’s disease. Its mechanism of action and biological activity provide insights into adenosine receptor modulation and its implications in neurodegenerative disorders. -
hA2AAR Antagonist
hA2AAR antagonist 1 is a highly selective antagonist for the human adenosine A2A receptor (hA2AAR) with a Ki value of 5 nM. This compound is instrumental for research in immune-oncology, providing valuable insights into the modulation of immune responses through adenosine signaling pathways. Its specificity and potency make it a suitable tool for studying cancer immunotherapy and related biological processes.
