2. Signaling Pathways
  3. GPCR/G Protein
  4. Adenosine Receptor

Adenosine Receptor

P1 receptor

Adenosine Receptor

Related Products

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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-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
    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-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-147545
    A1AR antagonist 6
    		Antagonist
    A1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 6.38 and a pKi of 7.13.
    A1AR antagonist 6
  • 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-B0153AS
    Ticlopidine-d4 hydrochloride
    		Inhibitor
    Ticlopidine-d4 (hydrochloride) is the deuterium labeled Ticlopidine hydrochloride. Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM.
    Ticlopidine-d<sub>4</sub> hydrochloride
  • 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-144116
    A1AR antagonist 2
    		Antagonist
    A1AR antagonist 2 (compound 18h) is a potent A1 adenosine receptor (AR) antagonist with Kis of 1.49, 10.2, and 50.1 nM for hA1, hA2A and hA2B, respectively.
    A1AR antagonist 2
  • HY-148076
    A2A receptor antagonist 3
    		Antagonist
    A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively.
    A2A receptor antagonist 3
  • HY-146979
    hA2A/hCA XII modulator 1
    		Antagonist
    hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.
    hA2A/hCA XII modulator 1
  • HY-149916
    A2AR-antagonist-1
    		Antagonist
    A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2).
    A2AR-antagonist-1
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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