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-159650
    EOS-984
    Inhibitor 99.98%
    EOS-984 is a highly potent and selective ENT1 (equilibrative nucleoside transporter 1) inhibitor. EOS-984 is designed to inhibit the immunosuppressive activity of adenosine and restore immune cell proliferation.
    EOS-984
  • HY-B1505
    Acefylline
    Antagonist 99.52%
    Acefylline, a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
    Acefylline
  • HY-103186
    MRS-1706
    Antagonist 98.07%
    MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.
    MRS-1706
  • HY-147400
    Sipagladenant
    Modulator 99.68%
    Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.
    Sipagladenant
  • HY-W010435
    Sulcatone
    Activator 99.80%
    Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis.
    Sulcatone
  • HY-119413
    9-Ethyladenine
    Antagonist 99.93%
    9-Ethyladenine is a precursor of competitive antagonists of adenosine receptors (A1, A2, A3), with no significant inhibitory effect on adenine phosphoribosyltransferase (APRT). 9-Ethyladenine derivatives have high affinity and selectivity for A1 (Ki=27 nM), A2A (Ki=46 nM), and A3 (Ki=86 nM) receptors. 9-Ethyladenine does not inhibit brain APRT activity, can be used in the study of adenosine receptor-related diseases (such as nervous system diseases) models.
    9-Ethyladenine
  • HY-147907
    Adenosine receptor inhibitor 1
    Inhibitor 98.29%
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
    Adenosine receptor inhibitor 1
  • HY-111809
    N6-Ethyladenosine
    Agonist 99.90%
    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.
    N6-Ethyladenosine
  • HY-103180
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
    Agonist 99.80%
    2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
  • HY-111082
    ISAM-140
    Inhibitor 99.85%
    ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM.
    ISAM-140
  • HY-103164
    (E)-8-(3-Chlorostyryl)caffeine
    Antagonist 99.4%
    (E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.
    (E)-8-(3-Chlorostyryl)caffeine
  • HY-106841
    Draflazine
    99.06%
    Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia.
    Draflazine
  • HY-124543
    MRS-1191
    Antagonist 99.22%
    MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells. MRS-1191 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MRS-1191
  • HY-148088
    M1069
    Antagonist 98.04%
    M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
    M1069
  • HY-103162
    ANR94
    Antagonist 98.91%
    ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease.
    ANR94
  • HY-19365
    AB-MECA
    Agonist 98.32%
    AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level.
    AB-MECA
  • HY-101139A
    Xanthine amine congener hydrochloride
    Antagonist 98.03%
    Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice.
    Xanthine amine congener hydrochloride
  • HY-B1742
    Proxyphylline
    Antagonist 99.93%
    Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline
  • HY-19842
    GS-9667
    Agonist 98.08%
    GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).
    GS-9667
  • HY-136661
    (-)-N6-Phenylisopropyl adenosine
    Agonist 99.45%
    (-)-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
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