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-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-B0153A
    Ticlopidine hydrochloride
    		Inhibitor 99.99%
    Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM.
    Ticlopidine hydrochloride
  • HY-A0181S1
    Adenosine monophosphate-15N5 dilithium
    		Agonist 99.50%
    Adenosine monophosphate-15N5 dilithium is the 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>15</sup>N<sub>5</sub> dilithium
  • HY-18939
    N6-Cyclohexyladenosine
    		Agonist 99.98%
    N6-Cyclohexyladenosine is a selective adenosine A1 receptor agonist (EC50 = 8.2 nM). N6-Cyclohexyladenosine enhances the activation of the PI3K/Akt/CREB/BDNF axis. N6-Cyclohexyladenosine promotes remyelination, induces sleep, and improves 3-NP-induced Huntington's disease. N6-Cyclohexyladenosine can be used in liver cancer research.
    N6-Cyclohexyladenosine
  • HY-B0004
    Doxofylline
    		Antagonist 99.40%
    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-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-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-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-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-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-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-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-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-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-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-18776
    A2AR-agonist-1
    		Agonist 99.90%
    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.
    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
  • 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-109139
    Taminadenant
    		Antagonist 99.84%
    Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response.
    Taminadenant
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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