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

Adenosine Receptor

P1 receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-109139A
    Taminadenant mesylate
    Antagonist
    Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating T cell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA.
    Taminadenant mesylate
  • HY-115765
    N6-Benzyl-5'-ethylcarboxamido adenosine
    Agonist
    N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.
    N6-Benzyl-5'-ethylcarboxamido adenosine
  • 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-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-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-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-122105
    JNJ-40255293
    Antagonist
    JNJ-40255293 is a high-affinity human A 2A receptor antagonist with a KiKi of 7.5 nM. JNJ-40255293 can be used in the research of neurodegenerative diseases such as Parkinson's disease.
    JNJ-40255293
  • 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-136661
    (-)-N6-Phenylisopropyl adenosine
    Agonist
    (-)-N6-phenylisopropyl adenosine (D-phenylisopropyladenosine) is a adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K+-evoked Ca2+ uptake with an IC50 value of 0.5 µM.
    (-)-N6-Phenylisopropyl adenosine
  • 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
  • HY-N2189R
    Swertisin (Standard)
    Antagonist
    Swertisin (Standard) is the analytical standard of Swertisin. This product is intended for research and analytical applications. Swertisin, a C-glucosylflavone isolated from Iris tectorum, is known to have antidiabetic, anti-inflammatory and antioxidant effects. Swertisin is an adenosine A1 receptor antagonist.
    Swertisin (Standard)
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