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-124543
    MRS-1191
    		Antagonist 99.22%
    MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells. MRS-1191 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MRS-1191
  • HY-119413
    9-Ethyladenine
    		Antagonist 99.93%
    9-Ethyladenine is a precursor of competitive antagonists of adenosine receptors (A1, A2, A3), with no significant inhibitory effect on adenine phosphoribosyltransferase (APRT). 9-Ethyladenine derivatives have high affinity and selectivity for A1 (Ki=27 nM), A2A (Ki=46 nM), and A3 (Ki=86 nM) receptors. 9-Ethyladenine does not inhibit brain APRT activity, can be used in the study of adenosine receptor-related diseases (such as nervous system diseases) models.
    9-Ethyladenine
  • HY-159650
    EOS-984
    		Inhibitor 99.98%
    EOS-984 is a highly potent and selective ENT1 (equilibrative nucleoside transporter 1) inhibitor. EOS-984 is designed to inhibit the immunosuppressive activity of adenosine and restore immune cell proliferation.
    EOS-984
  • HY-103162
    ANR94
    		Antagonist 98.91%
    ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease.
    ANR94
  • HY-147907
    Adenosine receptor inhibitor 1
    		Inhibitor 98.29%
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
    Adenosine receptor inhibitor 1
  • HY-111082
    ISAM-140
    		Inhibitor 99.85%
    ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM.
    ISAM-140
  • HY-103164
    (E)-8-(3-Chlorostyryl)caffeine
    		Antagonist 99.4%
    (E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.
    (E)-8-(3-Chlorostyryl)caffeine
  • 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 98.71%
    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 99.36%
    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-109139
    Taminadenant
    		Antagonist 99.84%
    Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response.
    Taminadenant
  • HY-110037
    MRS-3777 hemioxalate
    		Antagonist
    MRS-3777 hemioxalate is a selective adenosine A3 receptor antagonist.
    MRS-3777 hemioxalate
  • HY-103186
    MRS-1706
    		Antagonist 98.07%
    MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.
    MRS-1706
  • HY-101139A
    Xanthine amine congener hydrochloride
    		Antagonist 98.03%
    Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice.
    Xanthine amine congener hydrochloride
  • HY-19842
    GS-9667
    		Agonist 98.08%
    GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).
    GS-9667
  • HY-W010435
    Sulcatone
    		Activator 99.80%
    Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis.
    Sulcatone
  • HY-136661
    (-)-N6-Phenylisopropyl adenosine
    		Agonist 99.45%
    (-)-N6-phenylisopropyl adenosine (D-phenylisopropyladenosine) is a adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K+-evoked Ca2+ uptake with an IC50 value of 0.5 µM.
    (-)-N6-Phenylisopropyl adenosine
  • HY-103180
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
    		Agonist 99.80%
    2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Adenosine Receptor Isoform Comparison

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