2. Signaling Pathways
  3. GPCR/G Protein
  4. Adenosine Receptor

Adenosine Receptor

P1 receptor

Adenosine Receptor

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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.

Adenosine Receptor Isoform Specific Products:

Adenosine Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-148088
    M1069
    		Antagonist 99.52%
    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-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-B1742
    Proxyphylline
    		Antagonist 99.93%
    Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline
  • 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-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-103165
    PSB-0788
    		Antagonist 99.68%
    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
  • HY-20176
    2,4-Dichlorothieno[3,2-d]pyrimidine
    2,4-Dichlorothieno[3,2-d]pyrimidine is a thienopyrimidine scaffold and a key synthetic precursor, which is widely used for constructing 4-arylthieno[3,2-d]pyrimidine compounds. 2,4-Dichlorothieno[3,2-d]pyrimidine serves for the development of 4-arylthieno[3,2-d]pyrimidine-based human adenosine A2a receptor antagonists, as well as thienopyrimidine-based PI3K-α inhibitors. In addition, 2,4-Dichlorothieno[3,2-d]pyrimidine has potential application value in studies related to whipworm disease.
    2,4-Dichlorothieno[3,2-d]pyrimidine
  • HY-13236
    LUF6000
    		Agonist 98.46%
    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.
    LUF6000
  • 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
  • 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-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-19661
    Tecadenoson
    		Agonist 99.69%
    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
    Tecadenoson
  • HY-103174
    MRS1334
    		Antagonist 98.93%
    MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment. MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MRS1334
  • HY-103170
    LUF5834
    		Agonist 99.8%
    LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively.
    LUF5834
  • HY-103187
    HEMADO
    		Agonist 99.9%
    HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype. HEMADO is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HEMADO
  • HY-153897
    PSB-1901
    		Antagonist
    PSB-1901 is a potent A2B adenosine receptor (A2BAR) antagonist with Kis of 0.0835 nM and 0.131 nM for human and mouse A2BARs respectively. PSB-1901 can be used for the research of cancer.
    PSB-1901
  • HY-B0809S
    Theophylline-d6
    		Inhibitor 99.30%
    Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
    Theophylline-d<sub>6</sub>
  • HY-B0004S
    Doxofylline-d6
    		Antagonist 99.67%
    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>
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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