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-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-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-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-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-14409
    Lu AA41063
    		Antagonist
    Lu AA41063 is an adenosine A2A receptor antagonist that may be useful in the treatment of Parkinson's disease. Lu AA41063 has a Ki value of 5.9 nM and targets the human A2A receptor.
    Lu AA41063
  • 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-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-B1505G
    Acefylline (GMP)
    		Antagonist
    Acefylline (Theophyllineacetic acid) (GMP), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline (GMP) is a peptidylarginine deiminase (PAD) activator. Acefylline (GMP) is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline (GMP) can be used in asthma research.
    Acefylline (GMP)
  • HY-120090
    MRS1177
    		Antagonist
    MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.
    MRS1177
  • HY-185758
    LUF5437
    		Antagonist
    LUF5437 is a potent and selective adenosine A1 receptor antagonist with a rat Ki of 7.3 nM. LUF5437 can be used for research on cardiovascular and neurological diseases.
    LUF5437
  • HY-118455
    MRS1097
    		Antagonist
    MRS1097 is a potent antagonist of adenosine hA3 receptor, with the Ki of 100 nM.
    MRS1097
  • HY-144672
    A2A receptor antagonist 2
    		Antagonist
    A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM.
    A2A receptor antagonist 2
  • HY-171467
    MRS7799
    		Antagonist
    MRS7799 is a selective A 3 Adenosine Receptor antagonist agsinst human, mouse, and rat A3AR with Kds of 0.55, 3.74 and 2.80 nM, respectively. MRS7799 can be used in the study of neurodegeneration, cancer, ischemia of the heart and brain, autoimmune inflammatory diseases.
    MRS7799
  • HY-175195
    Adenosine receptor antagonist 6
    		Antagonist
    Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
    Adenosine receptor antagonist 6
  • HY-146457
    A3AR antagonist 1
    		Antagonist
    A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations.
    A3AR antagonist 1
  • HY-182432
    A3AR antagonist-7
    		Antagonist
    A3AR antagonist-7 is a conjugable human A3 adenosine receptor (A3AR) antagonist with a Ki value of 31.8 nM. A3AR antagonist-7 is applicable to the research of melanoma, breast cancer and colorectal cancer.
    A3AR antagonist-7
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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