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-139694
    hA3AR agonist 1
    		Agonist
    hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki value of 2.40 nM.
    hA3AR agonist 1
  • HY-158179
    A3AR agonist 3
    		Agonist
    A3AR agonist 3 (Compound 15A) is a A3 adenosine receptor (A3AR) agonist, with Ki and EC50 values of 2.27 and 0.20 nM for hA3 and cAMP, respectivelly. A3AR agonist 3 can be used for the research of neuroinflammation.
    A3AR agonist 3
  • HY-111295
    LAS38096
    		Antagonist
    LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
    LAS38096
  • HY-162787
    Adenosine receptor antagonist 5
    		Antagonist
    Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes.
    Adenosine receptor antagonist 5
  • HY-W782550
    FK-352
    		Antagonist
    FK-352 is a selective adenosine A1 receptor antagonist. FK-352 significantly improves intradialytic hypotension in chronic hemodialysis. FK-352 can be used for the study of intradialytic hypotension.
    FK-352
  • HY-110186
    PQ-69
    		Antagonist
    PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction.
    PQ-69
  • HY-A0181S4
    Adenosine monophosphate-13C10,15N5,d12 dilithium
    		Agonist
    Adenosine monophosphate-13C10,15N5,d12 (AMP-13C10,15N5,d12) dilithium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.
    Adenosine monophosphate-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub>,d<sub>12</sub> dilithium
  • HY-155184
    A3AR agonist 2
    		Agonist
    A3AR agonist 2 (Compound 19) a selective A3AR agonist (Ki: 22.1 nM). A3AR agonist 2 stimulates β-arrestin2 recruitment, with EC50 value of 4.36 nM. A3AR agonist 2 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions. A3AR agonist 2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    A3AR agonist 2
  • HY-B0809S1
    Theophylline-d3
    		Inhibitor
    Theophylline-d3 is deuterated 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-d<sub>3</sub>
  • HY-179248
    Adenosine receptor antagonist 7
    		Antagonist
    Adenosine receptor antagonist 7 is an orally active triple A1/A2A/A2B adenosine receptor antagonist with Ki values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC50 = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer.
    Adenosine receptor antagonist 7
  • HY-W791727
    7-Methyladenosine perchlorate
    		Agonist
    7-Methyladenosine perchlorate is a synthetic analog of adenosine with agonist activity at adenosine receptors. 7-Methyladenosine perchlorate is able to modulate cell signaling and is useful for studying adenosine-related biological processes. 7-Methyladenosine perchlorate can be used as a potential inhibitor in compound development.
    7-Methyladenosine perchlorate
  • HY-151139
    LJ-4517
    		Antagonist
    LJ-4517 is a potent A2AAR antagonist, with a Ki of 18.3 nM. LJ-4517 is potent in displacing the binding of [3H]ZM241385 (HY-19532) at WT A2AAR. LJ-4517 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LJ-4517
  • HY-175487
    A2AAR antagonist 4
    		Antagonist
    A2AAR antagonist 4 is an orally active A2A Adenosine receptor antagonist with a Ki of 0.36 nM and a KB of 1 nM at hA2AAR. A2AAR antagonist 4 fully inhibits hA2AAR and hA2bAR at 10 μM. A2AAR antagonist 4 can be used for research of cancer, such as MC38 tiumor.
    A2AAR antagonist 4
  • HY-145706
    A2A/A1 AR antagonist-1
    		Antagonist
    A2A/A1 AR antagonist-1 (compound 1a) is dual potent A2A/A1 AR antagonist with Kis of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke.
    A2A/A1 AR antagonist-1
  • HY-120652
    A3AR antagonist 3
    		Antagonist
    A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors.
    A3AR antagonist 3
  • HY-135501
    Bamifylline
    		Antagonist
    Bamifylline is a drug in the chemical class of xanthine that acts as a selective adenosine A1 receptor antagonist.
    Bamifylline
  • HY-105138
    (6R)-Naxifylline
    		Antagonist
    (6R)-Naxifylline ((6R)-BG9719) (ENX R-enantiomer) is the R-enantiomer of Naxifylline (HY-19240). (6R)-Naxifylline is a A1-adenosine antagonist with saluretic activity. (6R)-Naxifylline induces relaxation of spontaneous tone in guinea pig trachea.
    (6R)-Naxifylline
  • HY-123203
    CP-608039
    		Agonist
    CP-608039 is a potent and selective adenosine A3 receptor agonist. CP-608039 can be used for ischemic myocardial injury research.
    CP-608039
  • HY-161418
    1-NBX
    		Activator
    1-NBX is a potent and selective A1R ligand. 1-NBX exhibits significantly improved A1R affinity with with a Ki of 2.6 nM and lower affinity for the A2A receptor with a Ki of 164 nM.
    1-NBX
  • HY-133862
    SCH-202676
    		Modulator
    SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 µM.
    SCH-202676
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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