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2-Cl-IB-MECA (Chloro-IB-MECA, CF-102, Namodenoson) is a potent, selective A3 adenosine receptor agonist with Ki of 0.33 nM, 2500- and 1400-fold selectivity over A1 and A2a receptors; also displays 46,000-fold selectivity versus the Na(+)-independent adenosine transporter; inhibits adenylate cyclase via rat A3 receptors in CHO cells (IC50=67 nM); induces apoptosis in HL-60 cells at concentrations of <30 uM, significantly induced Ca(2+) release from intracellular Ca(2+) pools followed by Ca(2+) influx; increases plasma histamine concentrations in conscious rats.

Liver Cancer

Phase 2 Clinical



AZD-4635 (HTL 1071) is a potent, selective and orally available adenosine 2A receptor (A2AR) inhibitor with Ki of 1.7 nM, > 30-fold selectivity over other adenosine receptors; reverses the inhibitory effects of different concentrations of adenosine in CHO cells stably expressing human A2AR with IC50 of 0.1 nM (incubated with 0.1 uM adenosine); reverses suppression and restores IFNγ secretion in cells incubated with NECA in ex vivo CD8+ T cell assay; reduces tumor burden and enhances antitumor immunity in vivo.

Lung Cancer

Phase 2 Clinical



PBF509 (PBF-509, NIR 178) is a novel selective and potent Adenosine A2A Receptor (A2AR) antagonist, antagonizes A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 and 8.2 nM, respectively; PBF509 (orally) antagonized haloperidol-mediated catalepsy, reduced pilocarpine-induced tremulous jaw movements and potentiated the number of contralateral rotations induced by L-3,4-dihydroxyphenylalanine (L-DOPA) in unilaterally 6-OHDA-lesioned rats; PBF509 (3 mg/kg) inhibited L-DOPA-induced dyskinesia (LID), showing not only its efficacy on reversing parkinsonian motor impairments but also acting as antidyskinetic agent; increased responsiveness of human tumor-infiltrating lymphocytes when combined with anti-PD-1 or anti-PD-L1.

MSX-3 hydrate

261717-23-1 MSX-3 hydrate is a potent, specific adenosine A2A receptor (A2AR) antagonist.


2042563-95-9 TP455 (TP-455) is a highly potent, selective A2A adenosine receptor inverse agonist with IC50 of 1.9 nM in cyclic AMP assays in hA2A CHO cells; TP455 proved to be more potent than morphine in writhing and tail immersion tests in mice with ED50 of 0.0328 mg/kg, exhibits great analgesic activity with an ED50 of 0.134 ± 0.011 mg/kg and minimum effective dose of 0.01 mg/kg; antagonizes CGS 21680-induced cell proliferation in cancer cell lines, inhibits GS 21680-dependent pERK1/2, pJNK MAPK kinase, and pAKT activation.

BAY 60-6583

910487-58-0 BAY 60-6583 (BAY606583) is a potent, selective adenosine A2B receptor agonist with EC50 of 2.83 nM (murine A2BR); inhibits fMLP-stimulated superoxide production by either naive neutrophils,TNF-α-primed neutrophils, or neutrophils isolated from mice at 1-10 nM; increases fMLP-stimulated superoxide production at higher concentrations (>1 uM); exhibits cardioprotective activity, attenuates infarct size in mouse model of myocardial ischemia.

Neladenoson dalanate hydrochloride

1239235-25-6 Neladenoson dalanate is a potent, selective, orally acitve partial adenosine A1 receptor (A1AR) agonist (EC50=0.1 nM) for the treatment of chronic heart failure.

Heart Failure

Phase 2 Clinical

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