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-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[1].
    (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
  • HY-19310
    AMP-579
    		Agonist
    AMP-579 is an adenosine receptor agonist that primarily targets adenosine A1 and A2A receptors (with Ki values of 1.7 and 4.5 nM for the A1 receptor in rat brain and adipocytes, and a Ki value of 56 nM for the A2A receptor in rat brain). AMP-579 inhibits lipolysis, restores insulin-dependent glucose transport, and reduces heart rate through the activation of A1 receptors, while it induces vasodilation, particularly in coronary arteries, through the activation of A2A receptors (with an IC50 of 0.3 μM in porcine coronary arterial rings). AMP 579 shows potential for application in cardioprotection and the treatment of acute myocardial infarction.
    AMP-579
  • HY-W480392
    1,9-Dimethylxanthine
    1,9-Dimethylxanthine is an adenosine receptor antagonist that has the activity of blocking the effects of adenosine on the central nervous system. 1,9-Dimethylxanthine enhances nerve excitability by regulating the adenosine system. 1,9-Dimethylxanthine is used as a pharmacological tool in research to help explore physiological and pathological processes related to adenosine.
    1,9-Dimethylxanthine
  • HY-112840
    ST3932
    		Antagonist
    ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
    ST3932
  • HY-113608
    VCP171
    		Modulator
    VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain.
    VCP171
  • HY-112658
    p-Iodoclonidine hydrochloride
    		Inhibitor
    p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM.
    p-Iodoclonidine hydrochloride
  • HY-161717
    MRS5663
    		Agonist
    MRS5663 (Compound 3a) is an A3AR agonist, with an EC50 of 5.62 nM for β-arrestin2 recruitment assay. MRS5663 has a cytoprotective effect on skeletal muscle ischemia-reperfusion injury/claudication model.
    MRS5663
  • HY-120941
    LASSBio-1359
    		Agonist
    LASSBio-1359 is an adenosine A2A receptor agonist with vasodilatory and anti-inflammatory activities.
    LASSBio-1359
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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