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Adenosine A2A Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-103164
    (E)-8-(3-Chlorostyryl)caffeine

    		Adenosine Receptor Monoamine Oxidase Neurological Disease
    (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-124151
    Adenosine-2'-monophosphate

    2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate

    		 Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
    Adenosine-2'-monophosphate
  • HY-109139
    Taminadenant
    1 Publications Verification

    NIR178; PBF509

    		 Adenosine Receptor Neurological Disease Cancer
    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-19310
    AMP-579

    		Adenosine Receptor Cardiovascular Disease Metabolic Disease
    AMP-579 is an adenosine receptor agonist that primarily targets adenosine A1 and A2A receptors (with Ki values of 1.7 and 4.5 nM for the A1 receptor in rat brain and adipocytes, and a Ki value of 56 nM for the A2A receptor in rat brain). AMP-579 inhibits lipolysis, restores insulin-dependent glucose transport, and reduces heart rate through the activation of A1 receptors, while it induces vasodilation, particularly in coronary arteries, through the activation of A2A receptors (with an IC50 of 0.3 μM in porcine coronary arterial rings). AMP 579 shows potential for application in cardioprotection and the treatment of acute myocardial infarction .
    AMP-579
  • HY-147908
    Adenosine receptor inhibitor 2

    		Xanthine Oxidase Adenosine Receptor Inflammation/Immunology
    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-119191
    KF26777 free base

    		Adenosine Receptor Neurological Disease
    KF26777 (free base) is a potent and selective adenosine A3 receptor antagonist with an Ki value of 0.2 nM and possesses 9000-, 2350- and 3100-fold selectivity against adenosine A1, A2A and A2B receptors, respectively. KF26777 (free base) potently inhibits the [125I]AB-MECA binding to adenosine A3 receptors. KF26777 (free base) is promising for research of brain ischemia and inflammatory disease including asthma .
    KF26777 free base
  • HY-170397
    ADORA2A/PDE4D-IN-1

    		Phosphodiesterase (PDE) Adenosine Receptor Inflammation/Immunology
    ADORA2A/PDE4D-IN-1 (Compound 9) is a dual inhibitor for adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). ADORA2A/PDE4D-IN-1 can be used in research of bronchial asthma .
    ADORA2A/PDE4D-IN-1
  • HY-109139A
    Taminadenant mesylate

    NIR178 mesylate; PBF509 mesylate

    		 Adenosine Receptor Cancer
    Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating T cell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA .
    Taminadenant mesylate
  • HY-137370
    2-Hexynyl-5′-N-ethylcarboxamidoadenosine

    HENECA; 2-Hexynyl-NECA

    		 Adenosine Receptor Amyloid-β Neurological Disease
    2-Hexynyl-5′-N-ethylcarboxamidoadenosine (HENECA) is a selective A2A adenosine receptor agonist. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine increases intracellular cAMP level, and inhibits TNFα-evoked MMP-3 release. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine induces Aβ42 production in SH-SY5Y cells .
    2-Hexynyl-5′-N-ethylcarboxamidoadenosine
  • HY-120826
    A2AAR/hMAO-B-IN-1

    		Monoamine Oxidase Adenosine Receptor Neurological Disease
    A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
    A2AAR/hMAO-B-IN-1
  • HY-149916
    A2AR-antagonist-1

    		Adenosine Receptor Cancer
    A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
    A2AR-antagonist-1

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