2. Signaling Pathways
  3. GPCR/G Protein
  4. Adenosine Receptor

Adenosine Receptor

P1 receptor

Adenosine Receptor

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Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.

Adenosine Receptor Isoform Specific Products:

Adenosine Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103181
    N6-Cyclopentyladenosine
    		Agonist 99.95%
    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. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures.
    N6-Cyclopentyladenosine
  • HY-A0168
    Regadenoson
    		Agonist 99.59%
    Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS.
    Regadenoson
  • HY-101980
    Imaradenant
    		Antagonist 99.68%
    AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.
    Imaradenant
  • HY-N0092S2
    Inosine-13C5
    		Agonist 99.90%
    Inosine-13C5 is the 13C5 labeled Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors.
    Inosine-<sup>13</sup>C<sub>5</sub>
  • HY-W011012
    Adenosine 5'-monophosphate disodium
    		99.63%
    Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes.
    Adenosine 5'-monophosphate disodium
  • HY-12365
    Namodenoson
    		Agonist 99.56%
    Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
    Namodenoson
  • HY-121119
    MRS 1523
    		Antagonist 99.97%
    MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.
    MRS 1523
  • HY-103169
    SCH442416
    		Antagonist 99.94%
    SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
    SCH442416
  • HY-A0181A
    Adenosine 5'-monophosphate monohydrate
    		Agonist 99.07%
    Adenosine 5'-monophosphate monohydrate is an adenosine A1 receptor agonist. Adenosine 5'-monophosphate monohydrate has significant antiviral activity against HSV-1 and HSV-2.
    Adenosine 5'-monophosphate monohydrate
  • HY-100678
    CGS 15943
    		Antagonist 99.96%
    CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
    CGS 15943
  • HY-B0128
    Diphylline
    		Antagonist 99.22%
    Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator agent and has the potential for chronic bronchitis and emphysema.
    Diphylline
  • HY-101984
    N6,N6-Dimethyladenosine
    		Ligand 99.95%
    N6,N6-Dimethyladenosine, a modified ribonucleoside, is an endogenous A3 adenosine receptor ligand. N6,N6-Dimethyladenosine is an AKT inhibitor with antitumor effects. N6, N6-Dimethyladenosine targets SARS-CoV-2 entry protein ADAM17. N6, N6-Dimethyladenosine robustly inhibits AKT signaling in a variety of non-small cell lung cancer cell lines.
    N6,N6-Dimethyladenosine
  • HY-153152
    DPTN dihydrochloride
    		Antagonist 98.47%
    DPTN is a potent and selective human, mouse, and rat A3AR antagonist with Ki values of 1.65, 9.61, and 8.53 nM, respectively.
    DPTN dihydrochloride
  • HY-B0140
    Aminophylline
    		Antagonist 99.68%
    Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research.
    Aminophylline
  • HY-103182
    PSB-1115
    		Antagonist ≥99.0%
    PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh).
    PSB-1115
  • HY-110012
    SCH-202676 hydrobromide
    		Modulator
    SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 μM.
    SCH-202676 hydrobromide
  • HY-W017163
    7-Methylxanthine
    		Antagonist ≥99.0%
    7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity.
    7-Methylxanthine
  • HY-14858
    Derenofylline
    		Antagonist 99.93%
    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. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
    Derenofylline
  • HY-14917
    Capadenoson
    		Agonist 99.62%
    Capadenoson is a selective agonist of adenosine-A1 receptor.
    Capadenoson
  • HY-B0153A
    Ticlopidine hydrochloride
    		Inhibitor 99.99%
    Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM.
    Ticlopidine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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