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-123085
    Alloxazine
    Antagonist 98.98%
    Alloxazine is a selective A2b antagonist. Alloxazine completely block 5’N-Ethylcarboxamido adenosine (NECA)-mediated cyclic AMP accumulation with an IC50 of 2.9 μM. Alloxazine can be used for the research of cancer.
    Alloxazine
  • 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-103189
    VUF-5574
    Antagonist ≥99.0%
    VUF-5574 is a selective antagonist of adenosine A3 receptor with a Ki of 4.03 nM for the recombinant human receptor.
    VUF-5574
  • HY-14117
    Enprofylline
    Inhibitor 99.22%
    Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease.
    Enprofylline
  • HY-103175
    PSB36
    Antagonist ≥99.0%
    PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia.
    PSB36
  • HY-P99483
    Blontuvetmab
    Antagonist 99.08%
    Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma.
    Blontuvetmab
  • HY-13236
    LUF6000
    Agonist 99.09%
    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.
    LUF6000
  • HY-110037
    MRS-3777 hemioxalate
    Antagonist
    MRS-3777 hemioxalate is a selective adenosine A3 receptor antagonist.
    MRS-3777 hemioxalate
  • 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-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-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-W011955
    8-Cyclopentyl-1,3-dimethylxanthine
    Antagonist 99.82%
    8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor antagonist with Kis of 10.9 nM and 1440 nM for A1 receptor and A2 receptor, respectively.
    8-Cyclopentyl-1,3-dimethylxanthine
  • 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
  • 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-B0004S
    Doxofylline-d6
    Antagonist ≥99.0%
    Doxofylline-d6 is the deuterium labeled Doxofylline. Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
    Doxofylline-d<sub>6</sub>
  • HY-N0586
    Norisoboldine
    Agonist
    Norisoboldine is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
    Norisoboldine
  • HY-139314
    A2B receptor antagonist 2
    Antagonist 99.39%
    A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively.
    A2B receptor antagonist 2
  • 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-136233A
    PSB 0777 ammonium hydrate
    ≥99.0%
    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-147908
    Adenosine receptor inhibitor 2
    Inhibitor 99.08%
    Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR.
    Adenosine receptor inhibitor 2
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