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-10965
    Rolofylline
    Antagonist 99.68%
    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.
    Rolofylline
  • HY-128064
    Adenosine amine congener
    Agonist 99.23%
    Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. Adenosine amine congener also has neuroprotective effects.
    Adenosine amine congener
  • HY-106841
    Draflazine
    99.06%
    Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia.
    Draflazine
  • HY-10857
    Vipadenant
    Antagonist 98.02%
    Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
    Vipadenant
  • HY-102024
    A2A receptor antagonist 1
    Antagonist 99.88%
    A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively.
    A2A receptor antagonist 1
  • HY-148088
    M1069
    Antagonist 98.04%
    M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
    M1069
  • HY-111809
    N6-Ethyladenosine
    Agonist 99.90%
    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.
    N6-Ethyladenosine
  • HY-101300
    Cirazoline hydrochloride
    Agonist 99.65%
    Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM).
    Cirazoline hydrochloride
  • HY-19365
    AB-MECA
    Agonist 98.32%
    AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level.
    AB-MECA
  • HY-106450
    Binodenoson
    Agonist 98.01%
    Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging.
    Binodenoson
  • HY-N0092S
    Inosine-2,8-d2
    Agonist 99.69%
    Inosine-2,8-d2 is the deuterium labeled Inosine. 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.
    Inosine-2,8-d<sub>2</sub>
  • HY-N0586A
    Norisoboldine hydrochloride
    Agonist 99.72%
    Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
    Norisoboldine hydrochloride
  • HY-136233A
    PSB 0777 ammonium hydrate
    99.68%
    PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research.
    PSB 0777 ammonium hydrate
  • HY-106199
    Adenosine A1 receptor activator T62
    Activator 98.93%
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
    Adenosine A1 receptor activator T62
  • HY-B1505
    Acefylline
    Antagonist 99.52%
    Acefylline (Theophyllineacetic acid), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
    Acefylline
  • HY-B1742
    Proxyphylline
    Antagonist 99.93%
    Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline
  • HY-103183
    CV1808
    Agonist ≥98.0%
    CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively.
    CV1808
  • HY-14365
    TC-G 1004
    Antagonist 98.11%
    TC-G 1004 (compound 16j) is an orally active A2A adenosine receptor antagonist, with Ki values of 0.44 nM and 80 nM for hA2A and hA1, respectively.
    TC-G 1004
  • HY-105017
    Evodenoson
    Agonist 99.9%
    Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α).
    Evodenoson
  • HY-A0181S
    Adenosine monophosphate-13C10,15N5 dilithium
    Agonist ≥99.0%
    Adenosine monophosphate-13C10,15N5(AMP-13C10,15N5) is the 13C-labeled 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> dilithium
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