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-W017163
    7-Methylxanthine
    		Antagonist 99.94%
    7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity.
    7-Methylxanthine
  • HY-124151
    Adenosine-2'-monophosphate
    		Activator 99.91%
    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-14858
    Derenofylline
    		Antagonist 99.93%
    Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
    Derenofylline
  • HY-103185
    CCPA
    		Agonist 99.77%
    CCPA (2-Chloro-N6-cyclopentyladenosine) a highly selective A1 adenosine receptors agonist with a Ki of 0.4 nM. CCPA inhibits adenylate cyclase with an IC50 of 33 nM. CCPA exhibits anti-seizure and cardiacprotective activity. CCPA can be used for the research of seizure and myocardial infarction.
    CCPA
  • HY-153152
    DPTN dihydrochloride
    		Antagonist 98.47%
    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-137442
    Inupadenant
    		Antagonist 98.27%
    Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant can not cross BBB. Inupadenant can enhance the humoral immune response and has anti-tumor activity.
    Inupadenant
  • HY-N7844
    N6-Benzyladenosine
    		Agonist 99.72%
    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-N0092R
    Inosine (Standard)
    		Agonist
    Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors. In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR.
    Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation.
    Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes.
    In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice.
    Inosine (Standard)
  • HY-147400
    Sipagladenant
    		Modulator 99.68%
    Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.
    Sipagladenant
  • HY-10081
    GS-6201
    		Antagonist 98.47%
    GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
    GS-6201
  • HY-N2189
    Swertisin
    		Antagonist 99.54%
    Swertisin is an oral adenosine A1 receptor antagonist and an SGLT2 inhibitor. Swertisin has anti-diabetic, antioxidant properties, inhibits HBV, and improves cognitive and memory impairments in mice.
    Swertisin
  • HY-103175
    PSB36
    		Antagonist 99.94%
    PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation.
    PSB36
  • HY-116800
    FR194921
    		Antagonist 98.10%
    FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
    FR194921
  • HY-123085
    Alloxazine
    		Antagonist 99.46%
    Alloxazine is a selective A2b antagonist. Alloxazine completely block 5’N-Ethylcarboxamido adenosine (NECA)-mediated cyclic AMP accumulation with an IC50 of 2.9 μM. Alloxazine can be used for the research of cancer.
    Alloxazine
  • HY-103164
    (E)-8-(3-Chlorostyryl)caffeine
    		Antagonist 99.4%
    (E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.
    (E)-8-(3-Chlorostyryl)caffeine
  • HY-13201
    CGS 21680
    		Agonist 99.88%
    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM.
    CGS 21680
  • HY-B0004
    Doxofylline
    		Antagonist 99.97%
    Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.
    Doxofylline
  • HY-B0809R
    Theophylline (Standard)
    		Inhibitor
    Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline (Standard)
  • HY-107046
    UK-432097
    		Agonist 98.9%
    UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research.
    UK-432097
  • HY-14917
    Capadenoson
    		Agonist 98.43%
    Capadenoson is a selective agonist of adenosine-A1 receptor.
    Capadenoson
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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