Home GPCR & G Protein Adenosine Receptor

Adenosine Receptor

Isoform-selective Products

Adenosine Receptor Products

  • All (29)
  • Adenosine Receptor Inhibitors (2)
  • Adenosine Receptor Antagonists (17)
  • Adenosine Receptor Agonists (9)
  • Adenosine Receptor Modulator (1)
  • New Adenosine Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2153 CGS 21680 HCl CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
Clin Immunol, 2024, 266:110309
CNS Neurosci Ther, 2024, 30(5):e14726
Cell Rep Med, 2023, 4(9):101188
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.
EMBO J, 2024, 43(19):4324-4355
Nat Commun, 2023, 14(1):3364
Commun Biol, 2023, 6(1):1271
S1647 Adenosine Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond.
J Immunother Cancer, 2024, 12(11)e009805
Nat Commun, 2022, 13(1):5845
Cancer Res, 2022, canres.1707.2021
S8105 ZM241385 ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
Front Cell Dev Biol, 2022, 10:827714
Mol Biol Rep, 2021, 10.1007/s11033-021-07017-1
Cell Mol Immunol, 2020, 10
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
S2790 Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
Nat Commun, 2023, 14(1):3364
Immunology, 2022, 10.1111/imm.13493
Sci Rep, 2022, 12(1):4183
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
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
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
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. Namodenoson exerts an anti‑NASH effect mediated via the de‑regulation of the PI3K/NF‑κB/Wnt/β‑catenin signaling 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.
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina,PCR 5332) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.
S0272 Derenofylline (SLV320) Derenofylline (SLV320) is a selective and potent adenosine A1 antagonist with Ki of 1 nM. Derenofylline shows selective 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).
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.
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
E4632New 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.
S9608 Etrumadenant (AB928) Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively.
Natural Product Communications, 2022, 2022;17(10)
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. 5'-N-Ethylcarboxamidoadenosine 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). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.
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.
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.
EMBO J, 2024, 43(19):4324-4355
Nat Commun, 2023, 14(1):3364
Commun Biol, 2023, 6(1):1271
S8105 ZM241385 ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
Front Cell Dev Biol, 2022, 10:827714
Mol Biol Rep, 2021, 10.1007/s11033-021-07017-1
Cell Mol Immunol, 2020, 10
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
S2790 Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
Nat Commun, 2023, 14(1):3364
Immunology, 2022, 10.1111/imm.13493
Sci Rep, 2022, 12(1):4183
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
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
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. Derenofylline shows selective 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).
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
E4632New 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.
S9608 Etrumadenant (AB928) Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively.
Natural Product Communications, 2022, 2022;17(10)
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.
S2153 CGS 21680 HCl CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 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 β-N9-glycosidic bond.
J Immunother Cancer, 2024, 12(11)e009805
Nat Commun, 2022, 13(1):5845
Cancer Res, 2022, canres.1707.2021
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. Namodenoson exerts an anti‑NASH effect mediated via the de‑regulation of the PI3K/NF‑κB/Wnt/β‑catenin signaling 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.
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.
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.
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. 5'-N-Ethylcarboxamidoadenosine 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.
E0356 MIPS521

MIPS521 is a positive allosteric modulator of the A1R that exhibits analgesic efficacy in rats in vivo.
E4632New 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.

Choose Selective Adenosine Receptor Inhibitors

Tags: Adenosine Receptor inhibitor|Adenosine Receptor agonist|Adenosine Receptor activator|Adenosine Receptor inducer|Adenosine Receptor antagonist|Adenosine Receptor signaling pathway|Adenosine Receptor assay kit