Adenosine Receptor

Other GPCR & G Protein Inhibitors

• Featured Inhibitors
• Inhibitors (2)
• Modulator (1)
• Agonists (12)
• Agonists (17)

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
S2153	CGS 21680 HCl	CGS 21680 HCl is an adenosine A2 receptor agonist with an IC50 of 22 nM, exhibiting 140-fold over A1 receptor.	Clin Immunol, 2024, 266:110309 CNS Neurosci Ther, 2024, 30(5):e14726 Cell Rep Med, 2023, 4(9):101188
S1647	Adenosine	Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a ">-"N9-glycosidic bond.	Cancer Cell, 2025, 43(4):776-796.e14 J Infect, 2025, 90(4):106449 Nat Commun, 2025, 16(1):10378
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
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
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 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
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