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-U00251
    KFM19
    Antagonist 99.44%
    KFM19 is a potent, selective Adenosine receptor (A1-receptor) antagonist, with an IC50 of 50 nM.
    KFM19
  • HY-144419
    Adenosine receptor antagonist 3
    Antagonist 99.12%
    Adenosine receptor antagonist 3 is a potent antagonist of adenosine receptor. Adenosine receptor antagonist 3 has the potential for the research of cancer disease (extracted from patent WO2019233994A1, compound 1).
    Adenosine receptor antagonist 3
  • HY-137442A
    Inupadenant hydrochloride
    Antagonist 99.60%
    Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. Inupadenant hydrochloride can not cross BBB. Inupadenant hydrochloride can enhance the humoral immune response and has anti-tumor activity.
    Inupadenant hydrochloride
  • HY-W004425
    DMPX
    Antagonist 99.66%
    DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease.
    DMPX
  • HY-N12422
    A2AAR antagonist 2
    Antagonist 99.40%
    3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research.
    A2AAR antagonist 2
  • HY-148076
    A2A receptor antagonist 3
    Antagonist 99.46%
    A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively.
    A2A receptor antagonist 3
  • HY-102086
    MSX3
    Antagonist
    MSX3 is a potent antagonist of adenosine A2A that can reverse the effects of the dopamine antagonist Haloperidol (HY-14538) on effort-related decision making in a T-maze cost/benefit procedure.
    MSX3
  • HY-14390
    LAS101057
    Antagonist 99.92%
    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
    LAS101057
  • HY-10888R
    Istradefylline (Standard)
    Antagonist
    Istradefylline (Standard) is the analytical standard of Istradefylline. This product is intended for research and analytical applications. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
    Istradefylline (Standard)
  • HY-117184
    MSX-2
    Antagonist
    MSX-2 is A2A adenosine receptor antagonist, with Ki of 5 nM in human that plays an important role in Parkinson's disease.
    MSX-2
  • HY-148088A
    M1069 free base
    Antagonist 98.92%
    M1069 (free base) 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 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
    M1069 free base
  • HY-134555
    A3AR antagonist 4
    Antagonist 99.98%
    A3AR antagonist 4 (Compd 1) is an A3AR antagonist, with Ki values of 30.8 nM (hA3) and 203 nM (hA1), repectively. A3AR antagonist 4 (Compd 1) can be used for the study of cerebral ischemia.
    A3AR antagonist 4
  • HY-121453R
    Bamifylline hydrochloride (Standard)
    Antagonist
    Bamifylline (hydrochloride) (Standard) is the analytical standard of Bamifylline (hydrochloride). This product is intended for research and analytical applications. Bamifylline hydrochloride is a drug in the chemical class of xanthine that acts as a selective adenosine A1 receptor antagonist.
    Bamifylline hydrochloride (Standard)
  • HY-147544
    A1AR antagonist 5
    Antagonist
    A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11.
    A1AR antagonist 5
  • 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-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-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-183993
    A3AR antagonist-8
    Antagonist
    A3AR antagonist-8 is a selective A3 adenosine receptor antagonist with a Ki of 98 nM for human A3 adenosine receptor. A3AR antagonist-8 can be used for the research of glaucoma, chronic renal disease, acute renal ischemia and reperfusion injury, and cancer.
    A3AR antagonist-8
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