2. GPCR/G Protein
  3. Adenosine Receptor

Adenosine 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.

Adenosine Receptor Related Products (99):

Cat. No. Product Name Effect Purity
  • HY-19532
    ZM241385 Antagonist 99.26%
    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM[1][2][3].
  • HY-13201A
    CGS 21680 Hydrochloride Agonist
    CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
  • HY-101978
    CPI-444 Antagonist 99.94%
    CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses[1].
  • HY-103173
    5'-N-Ethylcarboxamidoadenosine Agonist
    5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
  • HY-129393
    AB928 Antagonist 99.79%
    AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities[1][2].
  • HY-115765
    N6-Benzyl-5'-ethylcarboxamido adenosine Agonist
    N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist[1].
  • HY-103183
    CV1808 Agonist
    CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively[1].
  • HY-103190
    MRS1220 Antagonist
    MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].
  • HY-101980
    AZD4635 Antagonist 99.68%
    AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors[1].
  • HY-103171
    BAY 60-6583 Agonist
    BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model[1][5].
  • HY-19533
    SCH 58261 Antagonist 99.71%
    SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively[1][2][3].
  • HY-B0809
    Theophylline Inhibitor 99.94%
    Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
  • HY-10888
    Istradefylline Antagonist 99.84%
    Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
  • HY-N0092
    Inosine Agonist
    Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors[1][2][3].
  • HY-14121
    MRS 1754 Antagonist 98.31%
    MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats[1].
  • HY-124543
    MRS-1191 Antagonist 98.57%
    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[1].
  • HY-12365
    Namodenoson Agonist 99.71%
    Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively[1][2].
  • HY-A0168
    Regadenoson Agonist 99.59%
    Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
  • HY-13591
    Piclidenoson Agonist 99.32%
    Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19[1][2][3][4].
  • HY-B0153A
    Ticlopidine hydrochloride Inhibitor 99.99%
    Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM.