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:

Cat. No. Product Name Effect Purity
  • HY-103173
    5'-N-Ethylcarboxamidoadenosine
    		Agonist 99.86%
    5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
  • 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.
  • 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.
  • 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.
  • HY-129393
    Etrumadenant
    		Antagonist 99.79%
    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.
  • HY-136233A
    PSB 0777 ammonium hydrate
    		≥99.0%
    PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research.
  • HY-137442A
    Inupadenant hydrochloride
    		Antagonist 99.60%
    Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. Inupadenant hydrochloride is not brain-penetrant. Inupadenant hydrochloride has potent anti-tumor activity.
  • HY-155183
    A3AR agonist 1
    		Agonist
    A3AR agonist 1 (Compound 12) is an A3AR agonist (Ki: 25.8 nM). A3AR agonist 1 stimulates β-arrestin2 recruitment, with an EC50 value of 5.17 nM. A3AR agonist 1 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, etc.
  • 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.
  • HY-13201A
    CGS 21680 Hydrochloride
    		Agonist 99.70%
    CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
  • HY-N0092
    Inosine
    		Agonist ≥98.0%
    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.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-12365
    Namodenoson
    		Agonist 99.75%
    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.
  • 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.
  • HY-13591
    Piclidenoson
    		Agonist 99.32%
    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.
  • 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.
  • 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.
Adenosine Receptor Isoform Comparison

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