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-N0092
    Inosine
    		Agonist 99.61%
    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
  • HY-103173
    5'-N-Ethylcarboxamidoadenosine
    		Agonist 99.86%
    5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
    5'-N-Ethylcarboxamidoadenosine
  • HY-13201A
    CGS 21680 Hydrochloride
    		Agonist 99.70%
    CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
    CGS 21680 Hydrochloride
  • HY-B0809
    Theophylline
    		Inhibitor 99.89%
    Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline
  • HY-19532
    ZM241385
    		Antagonist 99.26%
    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
    ZM241385
  • HY-19842
    GS-9667
    		Agonist 98.08%
    GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).
    GS-9667
  • HY-105017
    Evodenoson
    		Agonist 99.74%
    Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α).
    Evodenoson
  • HY-105068
    Apadenoson
    		Agonist
    Apadenoson is an adenosine analog with selective agonist activity for the adenosine A2a receptor and induces coronary vasodilatation.
    Apadenoson
  • HY-19533
    SCH 58261
    		Antagonist 99.78%
    SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.
    SCH 58261
  • HY-10888
    Istradefylline
    		Antagonist 99.70%
    Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
    Istradefylline
  • HY-100937
    DPCPX
    		Antagonist 99.02%
    DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
    DPCPX
  • HY-103171
    BAY 60-6583
    		Agonist 99.97%
    BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50?= 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.
    BAY 60-6583
  • HY-129393
    Etrumadenant
    		Antagonist 99.76%
    Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities.
    Etrumadenant
  • HY-101978
    Ciforadenant
    		Antagonist 99.85%
    Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
    Ciforadenant
  • 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-103166
    PSB-603
    		Antagonist ≥99.0%
    PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM.
    PSB-603
  • HY-14121
    MRS 1754
    		Antagonist 98.31%
    MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats.
    MRS 1754
  • 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-13591
    Piclidenoson
    		Agonist 99.28%
    Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.
    Piclidenoson
  • HY-103169
    SCH442416
    		Antagonist 99.68%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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