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-12099
    A3AR antagonist 2
    		Antagonist
    A3AR antagonist 2 (compound 18) is a potent Human A3 adenosine receptor antagonist with an Ki value of 4.54 nM.
    A3AR antagonist 2
  • HY-158057
    A2AR/A2BR antagonist 1
    		Antagonist
    A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death.
    A2AR/A2BR antagonist 1
  • HY-179671
    A3AR antagonist 6
    		Antagonist
    A3AR antagonist 6 (Compound 5p) is a selective A3AR antagonist with a Ki of 6.8 nM. A3AR antagonist 6 can be used in tumor research.
    A3AR antagonist 6
  • HY-170397
    ADORA2A/PDE4D-IN-1
    		Antagonist
    ADORA2A/PDE4D-IN-1 (Compound 9) is a dual inhibitor for adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). ADORA2A/PDE4D-IN-1 can be used in research of bronchial asthma.
    ADORA2A/PDE4D-IN-1
  • HY-180424
    SYAF080
    		Antagonist
    SYAF080 is a human A₂B adenosine receptor (hA₂B AdoR) antagonist with a Ki of 23.6 nM and a KB of 25.2 nM. SYAF080no relevant inhibition of human CYP450 cytochromes. SYAF080 can be used for the research of inflammation, metabolic and cardiovascular disease.
    SYAF080
  • HY-144115
    A1AR antagonist 1
    		Antagonist
    A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Kis of 2.08, 6.91, and 31.2 nM for hA1, hA2A and hA2B, respectively.
    A1AR antagonist 1
  • HY-175851
    A2AAR antagonist 5
    		Antagonist
    A2AAR antagonist 5 is a selective A2AAR antagonist. A2AAR antagonist 5 inhibits NECA-stimulated adenylyl cyclase activity in hA2AAR-expressing CHO cells with an IC50 value of 1863 nM. A2AAR antagonist 5 possesses strong free radical scavenging activity, with an EC50 value of 22.21 μM in the DPPH assay. A2AAR antagonist 5 exerts notable neuroprotective effects in in vitro cerebral ischemia models. A2AAR antagonist 5 can be used for the study of cerebral ischemia.
    A2AAR antagonist 5
  • HY-19240
    Naxifylline
    		Antagonist
    Naxifylline (BG9719; CVT-124) is a potent and selective A1-adenosine antagonist with Ki values of 0.67 and 0.45 nM for rat and cloned human A1-receptors, respectively. Naxifylline is a potassium-sparing diuretic for the study of edema associated with congestive heart failure.
    Naxifylline
  • HY-105275A
    FK 453
    		Antagonist 99.20%
    FK 453 (compound 1d) is a potent and selective adenosine A1 receptor antagonist with an IC50 value of 17.2 nM.
    FK 453
  • HY-147541
    A2A/A3 AR antagonist-1
    		Antagonist
    A2A/A3 AR antagonist-1 (compound 23) is a dual A2A/A3 adenosine receptor (AR) fluorescent ligand, with Kis of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively.
    A2A/A3 AR antagonist-1
  • HY-100961
    NPC 200
    		Antagonist
    NPC 200 is a potent and selective antagonist of Adenosine A1 Receptor. NPC 200 reverses NECA-induced left and right atrial depression with EC50s of 1.08 and 2.03 μM.
    NPC 200
  • HY-118678
    MRS1186
    		Antagonist
    MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM.
    MRS1186
  • HY-146456
    A1AR antagonist 3
    		Antagonist
    A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases.
    A1AR antagonist 3
  • HY-181877
    IHCH-3185
    		Antagonist
    IHCH-3185 is an orally active class I HDAC inhibitor (HDAC1 IC50 =102.9 nM) and A2AR antagonist (A2AR Ki =7.6 nM). IHCH-3185 reverses immune gene silencing by inducing histone acetylation and blocks the adenosine signaling pathway to relieve T-cell suppression. IHCH-3185 exhibits antiproliferative activity, induces cell cycle arrest, and significantly improves the tumor microenvironment. IHCH-3185 reduces the proportion of regulatory T cells, increases the CD8+/Treg ratio, and upregulates the expression of key factors such as H2-K1, Cxcl9 and Cxcl10. IHCH-3185 shows significant antitumor potential in CT26 and MC38 mouse tumor models and is suitable for related cancer research.
    IHCH-3185
  • HY-109718
    ATL-801
    		Antagonist
    ATL-801, an A2B receptor selective antagonist, ameliorates murine colitis.
    ATL-801
  • HY-146478
    A1/A3 AR antagonist 1
    		Antagonist
    A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
    A1/A3 AR antagonist 1
  • HY-174413
    A2AAR antagonist 3
    		Antagonist
    A2AAR antagonist 3 is a selective and potent A2A adenosine receptor (A2A AR) antagonist with an IC50 of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A2A AR. A2AAR antagonist 3 demonstrates favorable stability in rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.
    A2AAR antagonist 3
  • HY-110303
    Xanthine amine congener dihydrochloride
    		Antagonist
    Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.
    Xanthine amine congener dihydrochloride
  • HY-180423
    IRFI-165
    		Antagonist 98.0%
    IRFI-165 is a potent and selective A1 adenosine receptor antagonist with a Ki of 7.9 nM for rat A1 AR. IRFI-165 exhibies high selectivity versus A2A and A3 receptors. IRFI-165 induces antidepressant activity in vivo. IRFI-165 can be used for the research of psychiatric and neurological disorders.
    IRFI-165
  • HY-116042
    FSCPX
    		Antagonist 99.72%
    FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.
    FSCPX
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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