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-146457
    A3AR antagonist 1
    Antagonist
    A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations.
    A3AR antagonist 1
  • HY-106180
    DTI 0009
    Agonist
    DTI 0009 is a selective adenosine A1 receptor agonist used to reduce heart rate in patients with atrial fibrillation and to treat arrhythmias.
    DTI 0009
  • 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-W011012R
    Adenosine 5'-monophosphate disodium (Standard)
    Adenosine 5'-monophosphate (disodium) (Standard) is the analytical standard of Adenosine 5'-monophosphate (disodium). This product is intended for research and analytical applications. Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes.
    Adenosine 5'-monophosphate disodium (Standard)
  • HY-123353
    Neladenoson dalanate
    Agonist
    Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
    Neladenoson dalanate
  • HY-103179
    SDZ-WAG994
    Agonist
    SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation.
    SDZ-WAG994
  • HY-161718
    MRS8028
    Agonist
    MRS8028 is an agonist for A3 adenosine receptor (A3AR), which binds hA3AR with Ki of 2.44 nM. MRS8028 is potential for ameliorating ischemia and inflammatory diseases.
    MRS8028
  • 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-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-178783
    MRS8454
    Modulator
    MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). MRS8454 can significantly enhance the maximum effect of the standard agonist Cl-IB-MECA by approximately 286%-300%, and significantly reduce its EC50 value. MRS8454 effectively enhances the ability of A3AR agonists to inhibit the cAMP accumulation induced by Forskolin (HY-15371). MRS8454 can be used for the development of molecular probes.
    MRS8454
  • HY-122963
    Danshenol B
    Danshenol B is a diterpenoid. Danshenol B has strong aldose reductase (AR) inhibitory activity with IC50 value of 0.042μM. Danshenol B can be used for the research of diabetic related complication resulted by metabolic abnormality, such as cataracts, retinopathy, neuropathy, and nephropathy.
    Danshenol B
  • HY-B0809B
    Theophylline sodium acetate
    Inhibitor
    Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline sodium acetate
  • 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-163978
    YGZ-331
    Activator
    YGZ-331 is a sedative with a calming effect. YGZ-331 is a derivative of the adenosine nucleoside NGBA, which can increase GABA levels. YGZ-331 exerts a sedative-hypnotic effect by activating A1R and A2aR, and inhibiting CaMKII phosphorylation (pCaMKII) levels. YGZ-331 can reduce the spontaneous motor activity of mice.
    YGZ-331
  • HY-110202
    MRS5698
    Agonist
    MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis.
    MRS5698
  • HY-106841A
    (S)-Draflazine
    Inhibitor
    (S)-Draflazine ((-)-Draflazine) is the (S)-configuration of Draflazine (HY-106841). (S)-Draflazine is a potent blocker of nucleoside transport.
    (S)-Draflazine
  • 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-143325
    A2AAR/HDAC-IN-2
    Inhibitor
    A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor.
    A2AAR/HDAC-IN-2
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