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, 10.1038/s41586-025-09755-9
J Infect, 2025, 90(4):106449
Front Cell Dev Biol, 2022, 10:827714
Verified customer review of ZM241385
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
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)
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 (2020), 2023, 4(2):e242
Mol Cancer Res, 2019, 17(5):1166-1179
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 Immunol Immunother, 2024, 73(6):108
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00163-1
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
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.
Front Immunol, 2021, 12:687296
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.
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.
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.