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-161717
    MRS5663
    		Agonist
    MRS5663 (Compound 3a) is an A3AR agonist, with an EC50 of 5.62 nM for β-arrestin2 recruitment assay. MRS5663 has a cytoprotective effect on skeletal muscle ischemia-reperfusion injury/claudication model.
    MRS5663
  • HY-120941
    LASSBio-1359
    		Agonist
    LASSBio-1359 is an adenosine A2A receptor agonist with vasodilatory and anti-inflammatory activities.
    LASSBio-1359
  • HY-158181
    A3AR agonist 5
    		Agonist
    A3AR agonist 5 (Compound 6b) is a A3 adenosine receptor (A3AR) activator, with EC50 and Ki values of 0.14 nM and 6.36 nM for cAMP and hA3, respectively. A3AR agonist 5 can be used in pain and inflammatory research.
    A3AR agonist 5
  • HY-143683S
    Theophylline-13C2,d6
    Theophylline-13C2,d6 (1,3-Dimethylxanthine-13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). 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-<sup>13</sup>C<sub>2</sub>,d<sub>6</sub>
  • HY-B1505G
    Acefylline (GMP)
    		Antagonist
    Acefylline (Theophyllineacetic acid) (GMP), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline (GMP) is a peptidylarginine deiminase (PAD) activator. Acefylline (GMP) is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline (GMP) can be used in asthma research.
    Acefylline (GMP)
  • HY-143324
    A2AAR/HDAC-IN-1
    		Inhibitor
    A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.
    A2AAR/HDAC-IN-1
  • HY-120090
    MRS1177
    		Antagonist
    MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.
    MRS1177
  • HY-145308
    Heterobivalent ligand-1
    Heterobivalent ligand-1 (compound 26) is a heterobivalent ligand for the Adenosine A 2A-dopamine D 2 receptor heteromer (KDB1 A2AR=2.1 nM, KDB1 D2R= 0.13 nM).
    Heterobivalent ligand-1
  • HY-118455
    MRS1097
    		Antagonist
    MRS1097 is a potent antagonist of adenosine hA3 receptor, with the Ki of 100 nM.
    MRS1097
  • HY-W707554
    Ticlopidine hydrochloride-d6
    Ticlopidine hydrochloride-d6 is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). 0
    Ticlopidine hydrochloride-d<sub>6</sub>
  • HY-115494
    Neladenoson dalanate hydrochloride
    		Agonist
    Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
    Neladenoson dalanate hydrochloride
  • HY-156983
    MRS 5980
    MRS 5980 is an A3AR agonist with a Ki value of 0.7 nM. MRS 5980 has oral activity.
    MRS 5980
  • HY-155772
    LUF7690
    LUF7690 (Compound 9) is a clickable and covalent affinity-based probe (AfBP) that targets the human A3AR (hA3AR). LUF7690 can be used in the detection and characterization of the hA3AR in different types of granulocytes, among other cell types.
    LUF7690
  • HY-144672
    A2A receptor antagonist 2
    		Antagonist
    A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM.
    A2A receptor antagonist 2
  • HY-159889
    hA3AR agonist 2
    		Agonist
    hA3AR agonist 2 (compound 1h) is an A3AR agonist, with a Ki of 3.5 nM.
    hA3AR agonist 2
  • HY-170948
    A2AR modulator-1
    		Modulator
    A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4+ T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models.
    A2AR modulator-1
  • HY-171467
    MRS7799
    		Antagonist
    MRS7799 is a selective A 3 Adenosine Receptor antagonist agsinst human, mouse, and rat A3AR with Kds of 0.55, 3.74 and 2.80 nM, respectively. MRS7799 can be used in the study of neurodegeneration, cancer, ischemia of the heart and brain, autoimmune inflammatory diseases.
    MRS7799
  • HY-W782193
    Sulcatone-d5
    Sulcatone-d5 (6-Methyl-5-hepten-2-one-d5) is the deuterium labeled Sulcatone (HY-W010435). Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis.
    Sulcatone-d<sub>5</sub>
  • HY-175195
    Adenosine receptor antagonist 6
    		Antagonist
    Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
    Adenosine receptor antagonist 6
  • HY-A0168A
    Regadenoson hydrate
    		Agonist
    Regadenoson hydrate (NSC 169186) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson hydrate 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 hydrate
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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