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-103185A
    CCPA hemihydrate
    Agonist
    CCPA (2-Chloro-N6-cyclopentyladenosine) hemihydrate a highly selective A1 adenosine receptors agonist with a Ki of 0.4 nM. CCPA hemihydrate inhibits adenylate cyclase with an IC50 of 33 nM. CCPA hemihydrate exhibits anti-seizure and cardiacprotective activity. CCPA hemihydrate can be used for the research of seizure and myocardial infarction.
    CCPA hemihydrate
  • HY-108942
    ASP5854
    Antagonist
    ASP5854 is an orally active, blood-brain barrier permeable adenosine A1/A2a dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal A2a receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease.
    ASP5854
  • HY-19532S
    ZM241385-d7
    Antagonist
    ZM241385-d7 is a deuterated form of ZM241385 (HY-19532). ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.
    ZM241385-d<sub>7</sub>
  • HY-106186
    GW-493838
    Agonist
    GW-493838 is a potent Adenosine A1 (A1AR) agonist. GW-493838 has the potential for the research of neuropathic pain.
    GW-493838
  • HY-153333
    A1/A3 AR antagonist 3
    Antagonist
    A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases.
    A1/A3 AR antagonist 3
  • 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-122231
    MRS3558
    Agonist
    MRS3558 is a potent and selective A3AR agonist, with Ki values of 0.6 nM for humans and 0.9 nM for rats, making it suitable for research in the fields of neuropathic pain and anesthesia.
    MRS3558
  • HY-105003
    ST 1535
    Antagonist 99.80%
    ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
    ST 1535
  • HY-182340
    KF20274
    Antagonist
    KF20274 is an orally active adenosine A1 receptor antagonist. KF20274 increases the fecal pellet output in rats, and does not affect small intestinal propulsion or gastric emptying at defecation-increasing doses. KF20274 does not induce diarrhea at defecation-increasing doses. KF20274 can be used for the research of constipation.
    KF20274
  • HY-163701
    hA2AAR antagonist 1
    Antagonist
    hA2AAR antagonist 1 (compound 4a) is a highly selective hA2AAR antagonist with a Ki of 5 nM. hA2AAR antagonist 1 can be used in the study of immune-oncology.
    hA2AAR antagonist 1
  • 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-147543
    A1AR antagonist 4
    Antagonist
    A1AR antagonist 4 (compound 22) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.51 and a pKi of 6.29.
    A1AR antagonist 4
  • HY-173498
    AR ligand 40
    Antagonist
    AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonist activity. AR ligand 40 exhibits antiproliferative effect on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells with EC50s of 7, 10, 12, 13, 15 and 39 μM.
    AR ligand 40
  • HY-182782
    Analgesic agent-4
    Ligand
    Analgesic agent-4 is an adenosine A3AR ligand with analgesic/antinociceptive activity. Analgesic agent-4 inhibits writhing responses in mice and exhibits dose-dependent activity in the acetic acid (HY-Y0319)-induced mouse writhing model. Analgesic agent-4 can be used in the research of pain-related diseases.
    Analgesic agent-4
  • HY-103176
    PSB11 hydrochloride
    Antagonist
    PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM).
    PSB11 hydrochloride
  • HY-101139
    Xanthine amine congener
    Antagonist
    Xanthine amine congener is a non-selective adenosine receptor antagonist. Xanthine amine congener induces convulsions in mice.
    Xanthine amine congener
  • HY-109139A
    Taminadenant mesylate
    Antagonist
    Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating T cell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA.
    Taminadenant mesylate
  • HY-19130
    BW-534U87
    Agonist
    BW-534U87 is an orally active adenosine A1 receptor agonist and competitive adenosine deaminase (ADA) inhibitor (Ki=7 μM). BW-534U87 elevates brain adenosine levels and suppresses epileptiform activity. BW-534U87 demonstrate anticonvulsant efficacy in animal seizure models. BW-534U87 is promising for research of epilepsy and adenosine-related neuropsychiatric disorders.
    BW-534U87
  • HY-183239
    A2AR/A2BR antagonist 2
    Antagonist
    A2AR/A2BR antagonist 2 is a dual A2A/A2B adenosine receptor antagonist with selectivity for the A1 receptor. A2AR/A2BR antagonist 2 reverses adenosine-mediated T-cell immunosuppression in the tumor microenvironment. A2AR/A2BR antagonist 2 can be used in cancer-related research.
    A2AR/A2BR antagonist 2
  • HY-115765
    N6-Benzyl-5'-ethylcarboxamido adenosine
    Agonist
    N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.
    N6-Benzyl-5'-ethylcarboxamido adenosine
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