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-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-110037
    MRS-3777 hemioxalate
    Antagonist
    MRS-3777 hemioxalate is a selective adenosine A3 receptor antagonist.
    MRS-3777 hemioxalate
  • HY-W011955
    8-Cyclopentyl-1,3-dimethylxanthine
    Antagonist 99.82%
    8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor antagonist with Kis of 10.9 nM and 1440 nM for A1 receptor and A2 receptor, respectively.
    8-Cyclopentyl-1,3-dimethylxanthine
  • HY-102024
    A2A receptor antagonist 1
    Antagonist 99.88%
    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 99.52%
    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
  • HY-14365
    TC-G 1004
    Antagonist 98.11%
    TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for hA2A and hA1, respectively.
    TC-G 1004
  • HY-103165
    PSB-0788
    Antagonist 99.68%
    PSB-0788 is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 can be used for the research for chronic inflammatory lung diseases.
    PSB-0788
  • HY-103174
    MRS1334
    Antagonist 98.93%
    MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment. MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MRS1334
  • HY-153897
    PSB-1901
    Antagonist
    PSB-1901 is a potent A2B adenosine receptor (A2BAR) antagonist with Kis of 0.0835 nM and 0.131 nM for human and mouse A2BARs respectively. PSB-1901 can be used for the research of cancer.
    PSB-1901
  • HY-B0004S
    Doxofylline-d6
    Antagonist 99.67%
    Doxofylline-d6 is the deuterium labeled Doxofylline. Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
    Doxofylline-d<sub>6</sub>
  • HY-139314
    A2B receptor antagonist 2
    Antagonist 99.60%
    A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively.
    A2B receptor antagonist 2
  • HY-144064
    Adenosine receptor antagonist 2
    Antagonist 99.37%
    Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.
    Adenosine receptor antagonist 2
  • HY-10888S
    Istradefylline-13C,d3
    Antagonist 98.27%
    Istradefylline-13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
    Istradefylline-<sup>13</sup>C,d<sub>3</sub>
  • HY-122105
    JNJ-40255293
    Antagonist 98.45%
    JNJ-40255293 is a high-affinity human A 2A receptor antagonist with a KiKi of 7.5 nM. JNJ-40255293 can be used in the research of neurodegenerative diseases such as Parkinson's disease.
    JNJ-40255293
  • HY-103178
    MRE3008F20
    Antagonist 99.70%
    MRE3008F20 is a highly efficient, highly selective and radioactive adenosine A3 receptor (AA3R) antagonist (Ki=1.8 nM). MRE3008F20 effectively antagonises Cl-IB-MECA-induced cAMP production in resting lymphocytes with an IC50 value of 5 nM. MRE3008F20 can be used in the study of AA3R.
    MRE3008F20
  • HY-147545
    A1AR antagonist 6
    Antagonist 98.13%
    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-14873
    Tonapofylline
    Antagonist 98.99%
    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-W063197
    Adenosine receptor antagonist 4
    Antagonist 99.35%
    Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor.
    Adenosine receptor antagonist 4
  • HY-148954
    PBF-999
    Antagonist 98.89%
    PBF-999 is a phosphodiesterase10A (PDE-10A) and adenosine A2A receptor (A2AR) dual antagonist.
    PBF-999
Cat. No. Product Name / Synonyms Application Reactivity

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