Catalog No.
Product Name
Application
Product Information
Citations
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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. -
hA3AR Inhibitor
PSB-10 hydrochloride is a highly selective antagonist of the human adenosine A3 receptor (hA3AR), demonstrating a Ki value of 0.44 nM. It exhibits over 800-fold selectivity for hA3AR compared to other adenosine receptor subtypes, including rA1, rA2A, hA1, hA2A, and hA2B, with respective Ki values of 805, 6040, 1700, 2700, and 30000 nM. This compound has been shown to induce thermal hyperalgesia in mouse models, making it valuable for exploring pain pathways and adenosine receptor signaling in research. -
A1AR Antagonist
A1AR antagonist 4 is a potent and selective A1 adenosine receptor (A1AR) antagonist, exhibiting a pIC50 of 5.51 and a pKi of 6.29. This compound is valuable for studying the role of A1AR in various physiological processes and diseases. Its application extends to research on cardiovascular functions, neuroprotection, and metabolic regulation, making it a crucial tool for advancing understanding in these fields. -
A3 Adenosine Receptor Antagonist
PSB11 hydrochloride is a selective antagonist of the A3 adenosine receptor, exhibiting a high affinity with a Ki value of 2.3 nM. This compound demonstrates reverse excitatory activity, making it a valuable tool for investigating the physiological and pharmacological roles of the A3 receptor. It is suitable for research applications involving modulation of adenosine signaling pathways and its implications in various biological processes. -
Adenosine Receptor Antagonist
Xanthine amine congener is a non-selective antagonist of adenosine receptors. This compound is known to induce convulsions in murine models, making it a valuable tool for studying the physiological and pharmacological roles of adenosine signaling in the central nervous system. It can be utilized in research applications focused on neurological disorders and receptor pharmacology. -
Adenosine Receptor Antagonist
Taminadenant mesylate is a potent antagonist of the adenosine A2A receptor, exhibiting significant anti-tumor properties. It selectively binds to A2A receptors on T lymphocytes, thereby alleviating adenosine/A2A-mediated inhibition and promoting T cell-mediated immune responses against cancer cells. Additionally, Taminadenant mesylate has demonstrated efficacy in reducing hyperactivity in Parkinson's disease models by inhibiting L-DOPA-induced dyskinesias, making it a valuable reagent for research in both oncology and neuropharmacology. -
A3 Adenosine Receptor Agonist
N6-Benzyl-5'-ethylcarboxamido adenosine is a selective agonist for the A3 adenosine receptor. This compound exhibits biological activity by enhancing A3 receptor signaling, which is implicated in various physiological processes, including anti-inflammatory responses and cardioprotection. It is valuable for research applications exploring the role of A3 receptors in pharmacology and disease models. -
Adenosine Receptor Agonist
hA3AR agonist 1 is a potent agonist of the human A3 adenosine receptor (hA3AR), exhibiting a Ki value of 2.40 nM. This compound is valuable for studying the roles of hA3AR in various physiological processes and its potential therapeutic applications in areas such as inflammation and cancer. Researchers can utilize hA3AR agonist 1 to investigate receptor signaling pathways and to assess the compound's effects in relevant biological assays. -
A3AR Agonist
A3AR agonist 3 is a selective agonist of the A3 adenosine receptor (A3AR), exhibiting Ki and EC50 values of 2.27 nM and 0.20 nM for human A3 receptors and cAMP modulation, respectively. This compound is valuable for studies investigating the role of A3AR in neuroinflammation, providing insights into its potential therapeutic implications in neurodegenerative conditions. Its high potency and selectivity make it a powerful tool for research involving adenosine receptor signaling pathways. -
A2B Antagonist
LAS38096 is a selective antagonist of the A2B adenosine receptor, exhibiting a high affinity with a Ki value of 17 nM. Through its inhibition of A2B receptor activity, LAS38096 has demonstrated significant potential in modulating adenosine-mediated biological processes. This compound is suitable for research applications related to inflammation, cancer, and cardiovascular diseases where adenosine signaling plays a critical role. -
A3 AR Antagonist
MRS542 is a nucleoside antagonist of the A3 adenosine receptor (A3 AR) with a pKi of 8.74. In addition to its antagonistic properties, MRS542 functions as a partial agonist, with an effective concentration (pEC50) of 7.76, promoting β-arrestin translocation. This compound is valuable for investigating the role of A3 AR in cardiovascular diseases and related research applications. -
Biochemical Assay Reagent
7-Methyladenosine perchlorate is a synthetic analog of adenosine that acts as an agonist at adenosine receptors. This compound effectively modulates cellular signaling pathways, making it a valuable reagent for investigating adenosine-related biological processes. Additionally, 7-Methyladenosine perchlorate holds potential as a tool in compound development, particularly as an inhibitor for biochemical assays.
