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-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-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-183239
    A2AR/A2BR antagonist 2
    		Antagonist
    A2AR/A2BR antagonist 2 is a dual A2A/A2B adenosine receptor antagonist with selectivity for the A1 receptor. A2AR/A2BR antagonist 2 reverses adenosine-mediated T-cell immunosuppression in the tumor microenvironment. A2AR/A2BR antagonist 2 can be used in cancer-related research.
    A2AR/A2BR antagonist 2
  • 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-153157
    MRS542
    		Antagonist
    MRS542 is a nucleoside A3 AR antagonist with a pKi of 8.74. MRS542 also acts as a partial agonist (pEC50 = 7.76) in promoting β-arrestin translocation. MRS542 can be converted into an agonist by LUF6000 (HY-13236). MRS542 can be used for cardiovascular disease research.
    MRS542
  • 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-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-182714
    N 0840
    		Antagonist
    N 0840 is a neutral antagonist of adenosine A1 receptor (A1AR), with a Ki value of 279 nM in rats and 1185 nM in humans. N 0840 modulates adenosine A1 receptor to increase forskolin-induced cyclic 3′,5′-adenosine monophosphate production, with a GTP shift value close to 1. N 0840 can be used in studies of neuroprotection, cardiovascular/renal function[1].
    N 0840
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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