Catalog No.
Product Name
Application
Product Information
Citations
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human A3 adenosine receptor antagonist /Aurora inhibitor
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.- Amy H. Ide, .et al. , Mol Biol Cell, 2023, Jun 1;34(7):ar76 PMID: 37126397
- Hazheen K, .et al. , J Biol Chem, 2020, August 20 PMID: 32820050
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Adenosine kinase inhibitor
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
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A2A antagonist
Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease.- PU Hamor, .et al. , Prog Neuropsychopharmacol Biol Psychiatry, 2020, Dec 20;103:109979 PMID: 32470496
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Adenosine A2A Receptor Agonist
CGS 21680 is a specific adenosine A2A subtype receptor agonist.- Qian Wang, .et al. , Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
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Adenosine A3-R agonist
IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.- Sameshima T, .et al. , Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
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Adenosine A2A antagonist
ZM-241385 is a potent and highly selective Adenosine A2A-R antagonist, with a pA2 of 9.02 for Adenosine A2A-R in cardiac vasculature and selectivities of 1000, 91 and 500,000 over Adenosine A1-R, Adenosine A2B-R and Adenosine A3-R sites, respectively.- Sheng-Tao Hou, .et al. , Research Square, 2023, Sep 28
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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. -
adenosine A1 receptor antagonist
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. -
adenosine A1 receptor antagonist
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. -
A1 adenosine receptor agonist
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. -
A1 receptor agonist
N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM). -
A2AR/ENT1 agonist
A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1. -
adenosine A1 receptor antagonist
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure. -
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). -
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. -
A2A adenosine agonist
Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve? -
adenosine A2A/A1 receptor antagonist
A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively. -
Adenosine receptor inhibitor
N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor -
A2A Receptor Antagonist
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). - Tamsulosin hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
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A1 adenosine receptor agonist
Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. -
Adenosine A2A receptor antagonist
Preladenant is a potent and selective antagonist at the adenosine A2A receptor. -
human 5'-methylthioadenosine phosphorylase inhibitor
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. -
adenosine A2B receptors antagonist
CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases. -
A2A receptor antagonist
Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease. -
Adenosine Receptor agonist
Capadenoson is a selective agonist of adenosine-A1 receptor. -
Adenosine A3 receptor agonist
CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. -
Adenosine A1 receptor agonist
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively. -
adenosine A3 receptor antagonist
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM. -
Adenosine receptor agonist
N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively. -
A1 adenosine receptor agonist
N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
