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-109139
    Taminadenant
    		Antagonist 99.84%
    Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response.
    Taminadenant
  • HY-10995
    Tozadenant
    		Antagonist 98.30%
    Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.
    Tozadenant
  • HY-B0128
    Diphylline
    		Antagonist 99.25%
    Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator agent and has the potential for chronic bronchitis and emphysema.
    Diphylline
  • HY-10965
    Rolofylline
    		Antagonist 99.45%
    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.
    Rolofylline
  • HY-10857
    Vipadenant
    		Antagonist 98.02%
    Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
    Vipadenant
  • HY-18978
    GR79236
    		Agonist 99.79%
    GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.
    GR79236
  • HY-139644
    MIPS521
    		Agonist 99.65%
    MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.
    MIPS521
  • HY-18776
    A2AR-agonist-1
    		Agonist 99.05%
    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.
    A2AR-agonist-1
  • HY-111809
    N6-Ethyladenosine
    		Agonist 99.53%
    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-19365
    AB-MECA
    		Agonist 98.01%
    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-124151
    Adenosine-2'-monophosphate
    		Activator ≥98.0%
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
    Adenosine-2'-monophosphate
  • HY-103180
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
    		Agonist 99.79%
    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-14873
    Tonapofylline
    		Antagonist ≥98.0%
    Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure.
    Tonapofylline
  • HY-N7844
    N6-Benzyladenosine
    		Agonist 99.43%
    N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma-.
    N6-Benzyladenosine
  • HY-153152
    DPTN dihydrochloride
    		Antagonist 98.66%
    DPTN is a potent and selective human, mouse, and rat A3AR antagonist with Ki values of 1.65, 9.61, and 8.53 nM, respectively.
    DPTN dihydrochloride
  • HY-18687
    APNEA
    		Agonist 98.96%
    APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a potent, non-selective A3 adenosine receptor agonist.
    APNEA
  • HY-14390
    LAS101057
    		Antagonist 99.40%
    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
    LAS101057
  • HY-102024
    A2A receptor antagonist 1
    		Antagonist 99.96%
    A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively.
    A2A receptor antagonist 1
  • 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-B1742
    Proxyphylline
    		Antagonist 99.93%
    Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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