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-N0138S
    Theobromine-d6
    		Inhibitor 98.0%
    Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
    Theobromine-d<sub>6</sub>
  • HY-404647
    FK3453
    		Inhibitor
    FK3453 is a dual adenosine A1/A2 inhibitor and a TSLP inhibitor. FK3453 is also a substrate of aldehyde oxidase (AO). FK3453 can inhibit the production of TSLP and IL-33. FK3453 is useful for research on Parkinson’s disease and allergic disorders.
    FK3453
  • HY-145406
    IHCH-3064
    		Inhibitor
    IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
    IHCH-3064
  • HY-130054
    Theophylline L-lysine
    		Inhibitor
    Theophylline L-lysine (Lysine theophyllinate) is a soluble derivative of Theophylline (HY-B0809). Theophylline L-lysine is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline L-lysine inhibits PDE3 activity to relax airway smooth muscle. Theophylline L-lysine has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB into the nucleus. Theophylline L-lysine induces apoptosis. Theophylline L-lysine can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline L-lysine
  • HY-103177
    PSB-10 hydrochloride
    		Inhibitor
    PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice.
    PSB-10 hydrochloride
  • HY-184116
    A2AR/EGFR-IN-1
    		Inhibitor
    A2AR/EGFR-IN-1 is a dual A2AR/EGFR inhibitor, with an IC50 of 0.037 μM against A2AR and an IC50 of 8.37 μM against EGFR. A2AR/EGFR-IN-1 induces cell cycle arrest at S and G2/M phases. A2AR/EGFR-IN-1 upregulates the expression of TP53, Caspase3 and Bax, downregulates the expression of Bcl2, and promotes cell Apoptosis. A2AR/EGFR-IN-1 restores colon crypt structure in an azoxymethane (HY-111375)-induced colorectal cancer model in vivo. A2AR/EGFR-IN-1 can be used for research related to colorectal cancer.
    A2AR/EGFR-IN-1
  • HY-175653
    Androgen receptor ligand 2
    		Inhibitor
    Androgen receptor ligand 2 is a PROTAC target protein ligand that can be used to synthesize the PROTAC Androgen receptor degrader-1 (HY-175652).
    Androgen receptor ligand 2
  • HY-127141
    Cizolirtine citrate
    		Inhibitor
    Cizolirtine citrate (E-4018) is an analgesic agent. Cizolirtine citrate has significant analgesic and anti-hyperalgesic action in neuropathic pain models.
    Cizolirtine citrate
  • HY-182518
    MDL-102234
    		Inhibitor
    MDL-102234 is a potent and selective adenosine A1 receptor antagonist with a Ki value of 23.2 nM at the adenosine A1 receptor. MDL-102234 can be used for the study of cognition enhancement-related neural functions.
    MDL-102234
  • HY-B0809S1
    Theophylline-d3
    		Inhibitor
    Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). 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-d<sub>3</sub>
  • HY-112658
    p-Iodoclonidine hydrochloride
    		Inhibitor 99.61%
    p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM.
    p-Iodoclonidine hydrochloride
  • HY-143324
    A2AAR/HDAC-IN-1
    		Inhibitor
    A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.
    A2AAR/HDAC-IN-1
  • HY-B0809B
    Theophylline sodium acetate
    		Inhibitor
    Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline sodium acetate
  • HY-106841A
    (S)-Draflazine
    		Inhibitor
    (S)-Draflazine ((-)-Draflazine) is the (S)-configuration of Draflazine (HY-106841). (S)-Draflazine is a potent blocker of nucleoside transport.
    (S)-Draflazine
  • HY-143325
    A2AAR/HDAC-IN-2
    		Inhibitor
    A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor.
    A2AAR/HDAC-IN-2
  • HY-123196
    CVT-2759
    		Inhibitor
    CVT-2759 is a potent inhibitor of A1-ADOR, with the IC50 values of 0.18 μM and 9.5 μM to reduce the binding of [3H]CPX in the absence and presence of 1 mM GTP. CVT-2759 plays an important role in slowing AV nodal conduction and thereby ventricular rate without causing AV block, bradycardia, atrial arrhythmias, or vasodilation.
    CVT-2759
  • HY-100130R
    N-[(4-Aminophenyl)methyl]adenosine (Standard)
    		Inhibitor
    N-[(4-Aminophenyl)methyl]adenosine (Standard) is the analytical standard of N-[(4-Aminophenyl)methyl]adenosine (HY-100130). This product is intended for research and analytical applications. 0
    N-[(4-Aminophenyl)methyl]adenosine (Standard)
  • HY-107203S
    Propentofylline-d6
    		Inhibitor
    Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders.
    Propentofylline-d<sub>6</sub>
  • HY-N0127R
    Yohimbine Hydrochloride (Standard)
    		Inhibitor
    Yohimbine Hydrochloride Standard is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.
    Yohimbine Hydrochloride (Standard)
  • HY-U00180
    KF21213
    		Inhibitor
    KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors. KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM).
    KF21213
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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