Catalog No.
Product Name
Application
Product Information
Citations
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adenosine receptor antagonist
Taminadenant is an antagonist of adenosine receptor. -
AA3R antagonist
Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist. -
A2a receptor antagonist
SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders. -
Adenosine A2 receptor agonist
CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. -
A2 receptor antagonist
Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor. -
A2AR antagonist
AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. -
A1 adenosine receptors antagonist
Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 μM for platelets). -
Adenosine receptor antagonist
Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. -
Adenosine A Receptor agonist
2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively). -
Adenosine Receptor Agonist
N6-Benzyladenosine is an adenosine receptor agonist that demonstrates significant cytotoxic activity. It effectively induces apoptosis in cells and arrests the cell cycle at the G0/G1 phase, making it a valuable tool for studying cell proliferation and death. Additionally, N6-Benzyladenosine inhibits Toxoplasma gondii adenosine kinase, providing insights into its potential applications in antiparasitic research and glioma studies. -
A1 Adenosine Receptor Agonist
CCPA (2-Chloro-N6-cyclopentyladenosine) is a highly selective agonist for A1 adenosine receptors, demonstrating a Ki value of 0.4 nM. This compound effectively inhibits adenylate cyclase, with an IC50 of 33 nM. CCPA is relevant in studies investigating anti-seizure and cardioprotective effects, making it a valuable tool for research related to seizures and myocardial infarction. -
A1 Adenosine Teceptors Agonist
CCPA hemihydrate is a highly selective agonist of the A1 adenosine receptors, exhibiting a Ki value of 0.4 nM. It demonstrates preferential binding to the A1 receptor over the A2 receptor, with a Ki of 3900 nM. As a purine nucleoside analog, CCPA hemihydrate has demonstrated broad antitumor activity, particularly in the context of indolent lymphoid malignancies. Its anticancer effects are mediated through mechanisms such as inhibition of DNA synthesis and induction of apoptosis, making it valuable for research applications in cancer therapy. -
A1/A2A/A2B Adenosine Receptor Antagonist
Adenosine receptor antagonist 7 is a potent triple antagonist of A1, A2A, and A2B adenosine receptors, demonstrating Ki values of 1.5 nM, 0.6 nM, and 21 nM, respectively. It effectively inhibits cAMP production in A2AR-HEK293 cells with an IC50 of 0.8 nM. This compound enhances the infiltration of effector T cells and increases the CD8+/Treg ratio in conjunction with Avelumab. Adenosine receptor antagonist 7 is valuable for cancer research, particularly in the study of colon cancer. -
Adenosine Receptor Antagonist
Adenosine receptor antagonist 6 selectively targets the A2A adenosine receptor, exhibiting a Ki value of 19.18 nM. This compound inhibits NECA-mediated cAMP production with an IC50 of 0.089 μM and mitigates immunosuppressive effects by promoting IL-2 and IFN-γ secretion. Additionally, adenosine receptor antagonist 6 counteracts the immunosuppressive actions of adenosine on T-cell activation and cytokine release, demonstrating potential in inhibiting tumor growth in CT26/MC38 xenograft models. It is suitable for research focused on colon cancer. -
PTP4A3 Inhibitor
JMS-053 is a potent and reversible inhibitor of PTP4A3, with an IC50 value of 18 nM. This compound also exhibits significant inhibitory activity against PTP4A1 and PTP4A2, with IC50s of 50 nM and 53 nM, respectively. Additionally, JMS-053 demonstrates inhibition of CDC25B and DUSP3 with IC50 values of 92.6 nM and 207.6 nM, respectively. Through mechanisms such as interference with RhoA and STAT3/p38 signaling pathways, JMS-053 effectively suppresses tumor cell proliferation and migration, making it a valuable tool for investigating various cancers, including ovarian, breast, and colon cancer. -
Stable Isotope
Theophylline-d6 is a deuterium-labeled analog of Theophylline, primarily utilized as a stable isotope in research. Theophylline functions as a nonselective phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist, while also acting as an activator of histone deacetylase (HDAC). This compound is valuable in studies exploring cellular signaling pathways, pharmacology, and the biochemical mechanisms underlying various therapeutic effects. -
Stable Isotope
Adenosine-d-1 is a deuterium-labeled derivative of adenosine, an endogenous autacoid that interacts with four G protein-coupled receptors: A1, A2A, A2B, and A3. This stable isotope serves as a valuable tool for studying adenosine's diverse biological functions and its role in various physiological and pathological processes. Applications include pharmacological research, metabolic studies, and the investigation of signal transduction pathways mediated by adenosine receptors. -
PDE-10A/A2AR Antagonist
PBF-999 is a dual antagonist of phosphodiesterase 10A (PDE-10A) and adenosine A2A receptors (A2AR). This compound exhibits significant modulation of intracellular signaling pathways, contributing to its potential in neuroscience research, particularly in studying disorders such as schizophrenia and Parkinson's disease. PBF-999 may facilitate insights into the therapeutic effects of PDE-10A and A2A receptor signaling in cognitive and motor function. -
Adenosine Receptor Antagonist
CGH2466 dihydrochloride is an orally active antagonist of adenosine receptors A1, A2B, and A3, exhibiting IC50 values of 19 nM, 21 nM, and 80 nM, respectively. This compound also inhibits p38 MAPK with an IC50 ranging from 187 to 400 nM and phosphodiesterase type 4D with an IC50 of 22 nM. CGH2466 dihydrochloride demonstrates significant anti-inflammatory properties in both in vitro and in vivo models, making it a valuable tool for research in asthma and chronic obstructive pulmonary disease (COPD). -
hA3AR Probe
LUF7690 is a clickable and covalent affinity-based probe designed to target the human A3 adenosine receptor (hA3AR). This compound enables the detection and characterization of hA3AR in various granulocytes and other cell types, facilitating studies in receptor biology and signaling pathways. LUF7690 serves as a valuable tool for research applications focused on adenosine receptor functions and their roles in immunological responses. -
hA2A AR/hCA XII Inhibitor
hA2A/hCA XII modulator 1 is a potent inhibitor of the human A2A adenosine receptor (hA2AAR) and human carbonic anhydrase XII (hCA XII). It demonstrates high affinity with IC50 values of 6.4 nM for hA2AAR and 6.2 nM for hCA XII, while exhibiting selectivity against other adenosine receptor subtypes and carbonic anhydrases. This compound is valuable for cancer research, particularly in studies related to tumor microenvironment modulation and metabolic pathways involving adenosine signaling and carbonic anhydrase activity. -
Stable Isotope
Doxofylline-d4 is a deuterium-labeled derivative of Doxofylline, which functions primarily as an antagonist of the adenosine A1 receptor while also inhibiting phosphodiesterase IV. This reagent is valuable for studying pharmacokinetics and metabolic pathways in research involving adenosine receptor modulation and phosphodiesterase activity. Its stable isotope labeling allows for enhanced detection and quantification in various analytical applications. -
Adenosine Receptor Antagonist
Acefylline piperazine is an adenosine receptor antagonist known for its ability to activate peptidylarginine deiminase (PAD). This xanthine derivative exhibits significant bronchodilator and cardiac stimulant properties, while also inhibiting rat lung cAMP phosphodiesterase isoenzymes. As a result, Acefylline piperazine is a valuable tool in asthma research and studies exploring pulmonary function and cardiovascular effects. -
GPCRs/Adenosine Modulator
SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs), specifically targeting adenosine receptors (AR). This compound exhibits antiviral properties and effectively inhibits the 3CLpro enzyme in a time-dependent manner, with an IC50 value of 0.655 µM. SCH-202676 is valuable for research applications focusing on GPCR signaling pathways and the development of antiviral therapeutic strategies. -
Adrenergic Receptor
Bremazocine is a potent agonist of the kappa opioid receptor, demonstrating significant analgesic activity. It exerts its effects by enhancing the release of endogenous norepinephrine, leading to peripheral analgesia. Additionally, Bremazocine interacts with adenosine receptors, further contributing to its analgesic properties. Its peripheral analgesic effects are dose-dependent and may be influenced by nonselective α(2) adrenergic receptor antagonists, indicating a mechanism involving norepinephrine pathways. This compound is suitable for research applications focused on pain modulation and neuropharmacology. -
ADRA2A Antagonist
Yohimbic acid ethyl ester is a selective antagonist of the alpha-2 adrenergic receptor subtype ADRA2A, exhibiting an IC50 of 31 nM. This compound is significant for studies investigating the modulation of adrenergic signaling pathways and has potential applications in researching cardiovascular function and neuropharmacology. Its specificity for ADRA2A makes it a valuable tool for exploring therapeutic strategies targeting adrenergic receptor-related disorders. -
A3AR Agonist
MRS5698 is a selective agonist of the A3 adenosine receptor (A3AR), effectively activating Gi protein signaling pathways. With Kis of approximately 3 nM for both human and mouse A3AR, this compound is valuable for investigating mechanisms related to pain and psoriasis. Its specificity may facilitate research into therapeutic applications targeting inflammatory and pain-related disorders. -
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.
