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-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
  • HY-123203
    CP-608039
    		Agonist
    CP-608039 is a potent and selective adenosine A3 receptor agonist. CP-608039 can be used for ischemic myocardial injury research.
    CP-608039
  • HY-161418
    1-NBX
    		Activator
    1-NBX is a potent and selective A1R ligand. 1-NBX exhibits significantly improved A1R affinity with with a Ki of 2.6 nM and lower affinity for the A2A receptor with a Ki of 164 nM.
    1-NBX
  • HY-133862
    SCH-202676
    		Modulator 99.46%
    SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 µM.
    SCH-202676
  • HY-N2189R
    Swertisin (Standard)
    		Antagonist
    Swertisin (Standard) is the analytical standard of Swertisin. This product is intended for research and analytical applications. Swertisin, a C-glucosylflavone isolated from Iris tectorum, is known to have antidiabetic, anti-inflammatory and antioxidant effects. Swertisin is an adenosine A1 receptor antagonist.
    Swertisin (Standard)
  • HY-158180
    A3AR agonist 4
    		Agonist
    A3AR agonist 4 is an A3 adenosine receptor (A3AR) agonist (Ki: 1.24 nM for hA3AR). A3AR agonist 4 inhibits cAMP production with an EC50 of 0.17 nM. A3AR agonist 4 can be used for research of inflammation and pain.
    A3AR agonist 4
  • HY-14773S
    (Rac)-Mirabegron-d5
    		Agonist
    (Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist.
    (Rac)-Mirabegron-d<sub>5</sub>
  • HY-161810
    MRS8247
    		Modulator
    MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) that can also slow the dissociation rate of agonists.
    MRS8247
  • HY-172244
    Zaladenant
    		Antagonist
    Zaladenant is an adenosine receptor antagonist with antitumor effects.
    Zaladenant
  • HY-153149
    LJ-2698
    		Antagonist
    LJ-2698 is an orally active adenosine A3 receptor antagonist. LJ-2698 induces increased levels of anti-inflammatory cytokines in macrophages and significantly elevates the number of anti-inflammatory M2 macrophages in the lung. LJ-2698 prevents alveolar cavity enlargement, restores pulmonary function, inhibits matrix metalloproteinase activity and pulmonary cell apoptosis in the lung tissues of mice. LJ-2698 prevents renal injury, inhibits renal lipid accumulation, and increases PGC1α levels in renal tissues of mice with diabetic nephropathy. LJ-2698 is applicable to the research of emphysema and diabetic nephropathy.
    LJ-2698
  • HY-178958
    PPAR agonist 7
    PPAR agonist 7 is an orally active pan-PPAR agonist, demonstrating potent activation of all three subtypes, PPARα (EC50 = 1.51 μM), PPARδ (EC50 = 1.11 μM), and PPARγ (EC50 = 3.14 μM). PPAR agonist 7 significantly enhances glucose uptake in adipocytes while exhibiting minimal adipogenic activity. PPAR agonist 7 can suppress PPARγ Ser273 phosphorylation in white adipose tissue and upregulate insulin-sensitizing genes. PPAR agonist 7 does not cause weight gain or fluid retention in high-fat diet (HFD)/ Streptozotocin (HY-13753) (STZ)-induced type 2 diabetes mellitus (T2DM) models. PPAR agonist 7 has selective modulation of PPAR signaling pathways without activation of adipogenic gene programs. PPAR agonist 7 can be used for the study of diabetes.
    PPAR agonist 7
  • HY-151899
    A3AR modulator 1
    		Agonist
    A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [35S]GTPγS binding Emax.
    A3AR modulator 1
  • HY-183599
    MK-1088
    		Antagonist
    MK-1088 is an orally active A2A/A2B adenosine receptor antagonist with human A2A Ki of 0.31 nM, human A2B Ki 5.3 nM. MK-1088 blocks receptor downstream signaling, inhibits CREB phosphorylation and reverses adenosine-mediated immunosuppression. MK-1088 restores TNF−α release and enhances tumor immune surveillance. MK-1088 can be used for the research of cancer[1].
    MK-1088
  • HY-167905
    ATL444
    		Antagonist
    ATL444 is a adenosine receptor antagonist, with Ki values of 7.0, 2.5, 61.8, >1000 nM for rA1AR, rA2AAR, rA2BAR, rA3AR, respectively.
    ATL444
  • HY-14408
    Lu AA47070
    		Antagonist
    Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade.
    Lu AA47070
  • HY-182687
    MRS7469
    		Agonist
    MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pKi is 8.67, mouse pKi is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields.
    MRS7469
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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