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Adenosine Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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 Receptor.
Front Immunol, 2021, 12:687296
S5358 Regadenoson Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
S0498 Namodenoson (CF-102) Namodenoson (CF-102, 2-Cl-IB-MECA) is an orally bioavailable and selective agonist of the A3 adenosine receptor (A3AR) with Ki of 0.33 nM. This compound exerts an anti-NASH effect mediated via the de-regulation of the PI3K/NF-κB/Wnt/β-catenin signalling pathway.
E4032 5'-Deoxy-5'-(methylthio)adenosine 5'-Deoxy-5'-(methylthio)adenosine (Methylthioadenosine, MTA) is a naturally occurring sulfur-containing nucleoside produced by the decarboxylation of S-adenosylmethionine. This nucleoside is a potent agonist of adenosine receptors with Ki of 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively.
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 antagonises A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets).
E2985 Capadenoson Capadenoson (BAY 68-4986) is an orally bioavailable, non-nucleoside partial adenosine A1 receptor agonist that exhibits an anti-ischemic effect.
E4450 N6-Cyclopentyladenosine N6-Cyclopentyladenosine is an adenosine derivative and a potent adenosine receptor agonist with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively. It acts as an anticonvulsant and might exhibit protective actions against (AMPH)-induced seizures.
E0356 MIPS521

MIPS521 is a positive allosteric modulator of the A1R that exhibits analgesic efficacy in rats in vivo.
S5678 trans-Zeatin-riboside Zeatin Riboside is the most active and ubiquitous form of the naturally occurring cytokinins that promote cell division, stimulate shoot proliferation, inhibit root formation, slow the aging process, and activate gene expression and metabolic activity. Zeatin riboside has an immunomodulatory effect by agonizing the mammalian adenosine A2A receptor.
E4632 Taminadenant Taminadenant (NIR178, PBF509) is a non-xanthine and non-furan antagonist of adenosine A2A receptor (A2AR). It can antagonise 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.
E4626 BAY 60-6583 BAY 60-6583 is a non-purine and selective agonist of adenosine A2breceptor, with an EC50 of 3-10 nM for human A2breceptors and >10 μM for A1 and A2areceptors. It binds to adenosine A2breceptor in mice, rabbits, and dogs with Ki of 750 nM, 340 nM, and 330 nM, respectively. It also enhances the antitumor activity of chimeric antigen receptor-modified T cells.
S0838 NBMPR (S-(4-Nitrobenzyl)-6-thioinosine) NBMPR (S-(4-Nitrobenzyl)-6-thioinosine) is an inhibitor of ENT1 transporter that crosses the blood-brain barrier and is able to potentiate the neuroprotective effects of adenosine.
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.
S6347 5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. It acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.
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.
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina, PCR 5332) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). This compound is also an inhibitor of CYP2B6 with a Ki of 0.2 μM.
Nature, 2025, 10.1038/s41586-025-09755-9
E6040New Imiquimod maleate Imiquimod maleate (R 837 maleate) is a small-molecule salt derivative of maleic acid, isolated from the Imiquimod free base and is an immune response modifier, a potent and selective agonist of toll like receptor 7 (TLR7), an antagonist of adenosine A₂A receptor with a Ki of 2.16 μM, and an inhibitor of adenylyl cyclase activity, inducing antiviral proteins like cystatin A. It exhibits strong antitumoral and antiviral efficacy, making it effective for conditions such as COVID 19, HPV warts, molluscum contagiosum, actinic keratosis, basal and squamous cell carcinoma, Bowen's disease, and vulvar intraepithelial neoplasia.
E6039 Imiquimod hydrochloride Imiquimod hydrochloride (R 837 hydrochloride) is a small-molecule immune response modifier, a potent and selective agonist of toll like receptor 7 (TLR7), an antagonist of adenosine A₂A receptor with a Ki of 2.16 μM, and an inhibitor of adenylyl cyclase activity, inducing antiviral proteins like cystatin A. It exhibits strong antitumoural and antiviral efficacy, making it effective for conditions such as COVID 19, HPV warts, molluscum contagiosum, actinic keratosis, basal and squamous cell carcinoma, Bowen's disease, and vulvar intraepithelial neoplasia.