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-103166R
    PSB-603 (Standard)
    Antagonist
    PSB-603 (Standard) is the analytical standard of PSB-603 (HY-103166). This product is intended for research and analytical applications. PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM.
    PSB-603 (Standard)
  • HY-105275AR
    FK 453 (Standard)
    Antagonist
    FK 453 (Standard) is the analytical standard of FK 453 (HY-105275A). This product is intended for research and analytical applications. FK 453 (compound 1d) is a potent and selective adenosine A1 receptor antagonist with an IC50 value of 17.2 nM.
    FK 453 (Standard)
  • HY-W069173
    2-Thioadenosine
    Ligand
    2-Thioadenosine is a selective A1 adenosine receptor (A1AR) ligand with a Ki of 80.3 nM. 2-Thioadenosine shows very low affinity for the A2A, A2B and A3 adenosine receptor subtypes. 2-Thioadenosine acts as a precursor for the synthesis of fluorescent A3 adenosine receptor-selective agonists.
    2-Thioadenosine
  • HY-103173R
    5'-N-Ethylcarboxamidoadenosine (Standard)
    Agonist
    5'-N-Ethylcarboxamidoadenosine (Standard) is the analytical standard of 5'-N-Ethylcarboxamidoadenosine. This product is intended for research and analytical applications. 5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
    5'-N-Ethylcarboxamidoadenosine (Standard)
  • HY-103165R
    PSB-0788 (Standard)
    Antagonist
    PSB-0788 (Standard) is the analytical standard of PSB-0788 (HY-103165). This product is intended for research and analytical applications. PSB-0788 is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 can be used for the research for chronic inflammatory lung diseases.
    PSB-0788 (Standard)
  • HY-10965R
    Rolofylline (Standard)
    Antagonist
    Rolofylline (Standard) is the analytical standard of Rolofylline. This product is intended for research and analytical applications. 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 (Standard)
  • HY-124151R
    Adenosine-2'-monophosphate (Standard)
    Activator
    Bisphenol A diglycidyl ether (Standard) is the analytical standard of Bisphenol A diglycidyl ether. This product is intended for research and analytical applications. Bisphenol A diglycidyl ether is used as a stabilizer and embedding agent.
    Adenosine-2'-monophosphate (Standard)
  • HY-121453
    Bamifylline hydrochloride
    Antagonist
    Bamifylline hydrochloride is a drug in the chemical class of xanthine that acts as a selective adenosine A1 receptor antagonist.
    Bamifylline hydrochloride
  • HY-B0549AS
    Flavoxate-d4 (hydrochloride)
    Ligand
    Flavoxate-d4 hydrochloride (Rec-7-0040-d4) is the deuterium labeled Flavoxate hydrochloride. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca2+ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba2+ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.
    Flavoxate-d<sub>4</sub> (hydrochloride)
  • HY-103168
    XCC
    Antagonist
    XCC, 1,3,8-substituted xanthine derivative, is an adenosine receptor antagonist with Ki of 1.905 μM[1].
    XCC
  • HY-158882
    FLAC6
    FLAC6 is a potent fluorinated detergent that can be used to solubilize membrane proteins (the native adenosine receptor A2AR, a G protein-coupled receptor, and two native transporters AcrB and BmrA). FLAC6 can maintain the structural and functional integrity of different membrane proteins.
    FLAC6
  • HY-103169R
    SCH442416 (Standard)
    Antagonist
    SCH442416 (Standard) is the analytical standard of SCH442416. This product is intended for research and analytical applications. SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
    SCH442416 (Standard)
  • HY-U00341
    ST4206
    Antagonist
    ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research.
    ST4206
  • HY-U00321
    A2B receptor antagonist 1
    Antagonist
    A2B receptor antagonist 1 is a potent A2B adenosine receptor antagonist extracted from patent WO 2009157938 A1 EXAMPLE 9B.
    A2B receptor antagonist 1
  • HY-U00189
    Sch412348
    Antagonist
    Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
    Sch412348
  • 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
  • HY-U00226
    UP202-56
    Agonist
    UP202-56 is an adenosine analogue, which is an adenosinergic agonist.
    UP202-56
  • HY-U00143
    N-0861 racemate
    Antagonist
    N-0861 racemate is the racemate of N-0861. N-0861 is a selective adenosine A1 receptor antagonist.
    N-0861 racemate
Cat. No. Product Name / Synonyms Application Reactivity

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