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-103190
    MRS1220
    Antagonist 99.52%
    MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.
    MRS1220
  • 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-14917
    Capadenoson
    Agonist 99.62%
    Capadenoson is a selective agonist of adenosine-A1 receptor.
    Capadenoson
  • 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-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-10889
    Preladenant
    Antagonist 99.82%
    Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
    Preladenant
  • 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-A0181R
    Adenosine monophosphate (Standard)
    Agonist
    Adenosine monophosphate (Standard) is the analytical standard of Adenosine monophosphate (HY-A0181). This product is intended for research and analytical applications. Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.
    Adenosine monophosphate (Standard)
  • 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-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-139644
    MIPS521
    Agonist 98.21%
    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-10995
    Tozadenant
    Antagonist 99.17%
    Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.
    Tozadenant
  • 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-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 selectively binds to adenosine A1 over adenosine A2 receptors (Ki of 3900 nM). CCPA is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.
    CCPA
  • 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-A0181BS
    Adenosine monophosphate-13C10,15N5 disodium
    Agonist 99.24%
    Adenosine monophosphate-13C10,15N5 (AMP-13C10,15N5) disodium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.
    Adenosine monophosphate-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub> disodium
  • HY-18978
    GR79236
    Agonist 99.89%
    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-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-18776
    A2AR-agonist-1
    Agonist 99.90%
    A2AR-agonist-1 is a potent A2AR agonist and ENT1 inhibitor with Ki of 4.39 and 3.47 for A2AR and ENT1.
    A2AR-agonist-1
  • 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
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