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-105003
    ST 1535
    		Antagonist 99.80%
    ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
    ST 1535
  • HY-163701
    hA2AAR antagonist 1
    		Antagonist
    hA2AAR antagonist 1 (compound 4a) is a highly selective hA2AAR antagonist with a Ki of 5 nM. hA2AAR antagonist 1 can be used in the study of immune-oncology.
    hA2AAR antagonist 1
  • HY-103177
    PSB-10 hydrochloride
    		Inhibitor
    PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice.
    PSB-10 hydrochloride
  • HY-147543
    A1AR antagonist 4
    		Antagonist
    A1AR antagonist 4 (compound 22) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.51 and a pKi of 6.29.
    A1AR antagonist 4
  • HY-173498
    AR ligand 40
    		Antagonist
    AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonist activity. AR ligand 40 exhibits antiproliferative effect on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells with EC50s of 7, 10, 12, 13, 15 and 39 μM.
    AR ligand 40
  • HY-103176
    PSB11 hydrochloride
    		Antagonist
    PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM).
    PSB11 hydrochloride
  • HY-101139
    Xanthine amine congener
    		Antagonist
    Xanthine amine congener is a non-selective adenosine receptor antagonist. Xanthine amine congener induces convulsions in mice.
    Xanthine amine congener
  • 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-W178327
    8-Chloro caffeine
    		Inhibitor
    8-Chloro caffeine binds to adenosine receptors (Ki = 30 µM). 8-Chloro caffeine potentiates UV-induced chromosomal aberrations in Cl-I Chinese hamster embryonic lung cells. 8-Chloro caffeine is a derivative of the methylxanthine alkaloid caffeine.
    8-Chloro caffeine
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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