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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. -
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). -
Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. -
Adenosine receptor antagonist
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. -
pyrazolopyridine anxiolytic
Tracazolate is a pyrazolopyridine anxiolytic known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases. -
adenosine receptor antagonist
AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
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. -
PDE Inhibitor
Theophylline sodium acetate functions as a potent phosphodiesterase (PDE) inhibitor, specifically targeting PDE3 to promote the relaxation of airway smooth muscle. It also acts as an adenosine receptor antagonist and histone deacetylase (HDAC) activator, contributing to its anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation to the nucleus. Additionally, Theophylline sodium acetate is known to induce apoptosis, making it a valuable reagent for research on asthma and chronic obstructive pulmonary disease (COPD). -
Stable Isotope
Theophylline-d3 is a deuterated form of theophylline, primarily used as a stable isotope in research applications. Theophylline functions as a potent phosphodiesterase inhibitor and adenosine receptor antagonist, contributing to its ability to relax airway smooth muscle. Additionally, it demonstrates anti-inflammatory effects by enhancing IL-10 production and inhibiting NF-κB nuclear translocation. This compound is valuable for studying asthma and chronic obstructive pulmonary disease (COPD) mechanisms and therapies. -
Stable Isotope
Theophylline-13C2,d6 is a stable isotope-labeled form of Theophylline (1,3-Dimethylxanthine), primarily acting as a phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist. This reagent enhances anti-inflammatory responses by increasing IL-10 levels and inhibiting NF-κB nuclear translocation, while also promoting apoptosis. It serves as a valuable tool for research into airway smooth muscle relaxation and the treatment of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). -
A2AAR/HDAC Dual Inhibitor
A2AAR/HDAC-IN-2 is a potent dual inhibitor targeting the adenosine A2A receptor (A2AAR) and histone deacetylase 1 (HDAC1). It demonstrates a strong binding affinity for A2AAR with a Ki value of 10.3 nM and exhibits significant inhibitory activity against HDAC1 with an IC50 of 18.5 nM. This compound is applicable in cancer research, particularly in studies exploring antitumor mechanisms and therapeutic efficacy. -
A2AAR/HDAC Inhibitor
A2AAR/HDAC-IN-1 is a potent dual inhibitor targeting the A2A adenosine receptor (A2AAR) and histone deacetylase 1 (HDAC1), with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. This compound demonstrates significant anticancer activity, making it a valuable reagent for research in cancer therapeutics and epigenetic modulation. Its oral bioavailability enhances its utility in in vivo studies, facilitating investigations into the mechanisms underlying tumor growth and proliferation. -
PARP-1 Inhibitor
Benzo[c][1,8]naphthyridin-6(5H)-one is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) and aurora kinase A, exhibiting IC50 values of 0.311 μM and 5.5 μM, respectively. This compound demonstrates low micromolar affinity for human adenosine receptors AR A1 and hA2A, with Ki values of 4.6 and 4.8 μM. Due to its mechanistic action, Benzo[c][1,8]naphthyridin-6(5H)-one is valuable for research applications targeting DNA repair pathways and cancer therapies. -
A2A Receptor/HDAC Inhibitor
IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications. -
Antibiotic
Adenoregulin, also known as Dermaseptin b2, is an antimicrobial peptide antibiotic that targets a broad spectrum of microorganisms. It exhibits activity against both Gram-negative and Gram-positive bacteria, as well as yeast and fungi. Additionally, Adenoregulin enhances the binding of agonists to the A1 adenosine receptor, making it valuable for research applications in microbiology and pharmacology. -
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. -
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. -
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. -
Adenosine Analog
N6-Benzoyl-7'-O-DMT-morpholino adenine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits notable biological activities, including smooth muscle vasodilation and the potential inhibition of cancer progression. It is commonly utilized in research applications related to cardiovascular studies and cancer therapeutics, contributing valuable insights into adenosine signaling and its effects on physiological processes. -
Adenosine Analog
2-Cyanomethylthioadenosine is an adenosine analog that primarily targets adenosine receptors. This compound demonstrates potent vasodilatory effects on smooth muscle tissue and has shown potential in inhibiting cancer progression. It serves as a valuable tool in research applications focusing on vascular biology and cancer therapeutics. -
Adenosine Analog
3’-β-C-Ethynyladenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. Additionally, this compound serves as a click chemistry reagent, featuring an alkyne group that allows it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation applications in chemical biology and drug development. -
Adenosine Analog
7'-O-DMT-morpholino thymine is an adenosine analog primarily known for its role in modulating adenosine receptors. It exhibits biological activities such as smooth muscle vasodilation and may play a role in inhibiting cancer progression. This compound is valuable for research applications in cardiovascular studies and cancer biology, providing insights into cellular signaling pathways and therapeutic strategies. -
Adenosine Analog
N6,N6-Dimethyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects on smooth muscle and has been implicated in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular studies and cancer biology, providing insights into the modulation of adenosine signaling pathways. -
Adenosine Analog
N6-(3-Methoxybenzyl)-2’-C-methyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and demonstrates potential anti-cancer properties. It is suitable for research applications focused on vascular biology and cancer therapeutics. -
Adenosine Analog
N6-Methyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound has demonstrated vasodilatory effects on smooth muscle and exhibits potential in inhibiting cancer progression. Its unique structure allows for various research applications related to adenosine signaling pathways and therapeutic interventions. -
Adenosine Analog
5’-O-(4,4’-Dimethoxytrityl)-N6-phenoxyacetyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. It is a valuable reagent for research focused on vascular biology, immunology, and oncology, facilitating investigations into the therapeutic potential of nucleotide derivatives. -
Adenosine Analog
5'-O-[Bis(4-methoxyphenyl)phenylmethyl]-adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for cancer research. It serves as a useful tool in studies focused on adenosine receptor modulation and vascular biology. -
Adenosine Analog
3’-O-Propargyladenosine is an adenosine analog that primarily targets adenosine receptors, acting as a vasodilator and exhibiting potential anti-cancer properties. It serves as a valuable tool in research applications involving click chemistry, due to its alkyne functional group, which facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This compound is instrumental in the study of biochemical pathways and therapeutic interventions related to adenosine signaling and vascular biology. -
Adenosine Analog
N6-Bz-5'-O-DMTr-3'-deoxyadenosine-2'-O-CED-phosphoramidite is an adenosine analog that primarily targets adenosine receptors. It exhibits biological activities such as smooth muscle relaxation and has demonstrated potential in inhibiting cancer progression. This compound is useful in various research applications, particularly in the development of nucleic acid-based therapeutics and the study of adenosine receptor signaling pathways. -
Adenosine Analog
5’-O-(4,4’-Dimethoxytrityl)-2’-beta-C-methyl adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound exhibits significant biological activities, including the inhibition of cancer progression. It serves as a valuable tool in research applications related to cardiovascular research, cancer therapies, and the study of adenosine receptor signaling pathways. -
Adenosine Analog
N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. This compound is valuable for research applications focusing on vascular biology, oncology, and the investigation of adenosine signaling pathways. -
Adenosine Analog
N-[[4-(Trifluoromethyl)phenyl]methyl]adenosine is an adenosine analog known for its smooth muscle vasodilatory effects. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for research in oncology and cardiovascular studies. Its biological activity positions it as a key reagent for investigating adenosine receptor pathways and their implications in various therapeutic contexts. -
Adenosine Analog
8-Benzyloxyadenosine is an adenosine analog that primarily targets adenosine receptors to elicit biological responses. This compound exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular biology and cancer therapeutics. -
Adenosine Analog
5-Methyl-4’-thiouridine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects, promoting smooth muscle relaxation, and has shown potential in inhibiting cancer progression. Its applications in research encompass studies on cardiovascular function and cancer therapeutics.

