Home GPCR & G Protein Adenosine Receptor

Adenosine Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S7588 Reversine Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 400 nM/500 nM/400 nM, respectively. Also used for stem cell dedifferentiation.
Nat Cell Biol, 2025, 27(1):59-72
EMBO J, 2024, 43(19):4324-4355
Sci Adv, 2024, 10(44):eado6607
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S8105 ZM241385 ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
Nature, 2025, 423-431
Nature, 2025, 10.1038/s41586-025-09755-9
J Infect, 2025, 90(4):106449
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S2790 Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
J Infect, 2025, 90(4):106449
Sci Adv, 2025, 11(9):eadq1724
Nat Commun, 2023, 14(1):3364
Verified customer review of Istradefylline
S8104 SCH58261 SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
CNS Neurosci Ther, 2024, 30(5):e14726
Molecules, 2022, 27(19)6267
J Neurochem, 2021, 10.1111/jnc.15436
S6646 Ciforadenant (CPI-444) Ciforadenant (CPI-444, V81444) is a potent and selective Adenosine A2A receptor antagonist. It binds to A2A receptors with a Ki of 3.54 nmol/L and demonstrates a greater than 50-fold selectivity for the A2A receptor over other adenosine receptor subtypes.
Cancer Immunology, Immunotherapy, April 20, 2024, 108
Nature Immunology, 2025, 854-865
Cancer Immunology, Immunotherapy, 2024, 108
S8575 A2AR antagonist 1 A2AR antagonist 1 is a potent A2AR (Adenosine A2A Receptor) antagonist with Ki values of 4 nM and 264 nM for A2AR and A1R, respectively.
MedComm, 2023, e242
MedComm (2020), 2023, 4(2):e242
Mol Cancer Res, 2019, 17(5):1166-1179
S9608 Etrumadenant (AB928) Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist, with Kd values of 1.4 nM and 2 nM for A2aR and A2bR, respectively.
FEBS Open Bio, 2025, 15(2):335-345
Nat Prod Commun, 2022, 17(10): 1–8
Natural Product Communications, 2022, 2022;17(10)
S8720 Imaradenant (AZD4635) Imaradenant (AZD4635, HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
Nature Immunology, 2025, Online ahead of print
Frontiers in Immunology, 2021, 687296
Front Immunol, 2021, 12:687296
E1310 DPCPX DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective adenosine A1 receptor (ADORA1) antagonist, with a Ki of 0.46 nM.
Cell Biol Toxicol, 2024, 40(1):59
S2945 SCH-442416 SCH-442416 is a selective antagonist of adenosine A2A receptor that binds to human and rat adenosine A2A receptors with Ki of 0.048 nM and 0.5 nM, respectively.
Blood Advances, 2025, 5423-5435
S0272 Derenofylline (SLV320) Derenofylline (SLV320) is a selective and potent adenosine A1 antagonist with Ki of 1 nM, and it shows selectivity for adenosine A1 over A2A, A2B, and A3 receptors with Ki of 398 nM, 3981 nM, and 200 nM, respectively.
S4932 Proxyphylline Proxyphylline (Monophylline, Spasmolysin) is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets).
E4632 Taminadenant Taminadenant (NIR178, PBF509) is a non-xanthine and non-furan antagonist of adenosine A2A receptor (A2AR). It can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with Kb values of 72.8 nM and 8.2 nM, respectively. It exhibits potential utility for Parkinson’s disease (PD) treatment.
S6639 BAY-545 BAY-545 is an A2B adenosine receptor antagonist with ic50 of 59 nM.
S6910 Preladenant Preladenant (Privadenant, SCH 420814, MK-3814) is a potent, competitive and selective antagonist of the human adenosine A2A receptor with Ki of 1.1 nM.
S5427 Alloxazine Alloxazine (Isoalloxazine) is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.
S3988 Theophylline-7-acetic acid Theophylline-7-acetic acid (Acefylline, acetyloxytheophylline, Carboxymethyltheophylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.