Adenosine Receptor

Choose Selective Adenosine Receptor Inhibitors

Adenosine Receptor Products

  • All (24)
  • Adenosine Receptor Inhibitors (2)
  • Adenosine Receptor Antagonists (15)
  • Adenosine Receptor Agonists (6)
  • Adenosine Receptor Modulator (1)
  • New Adenosine Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) 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 S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) S-(4-Nitrobenzyl)-6-thioinosine (NBMPR, Nitrobenzylthioinosine, NBTI, NSC 296962) is an inhibitor of ENT1 transporter that crosses the blood-brain barrier and is able to potentiate the neuroprotective effects of adenosine.
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.
S2790 Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
Immunology, 2022, 10.1111/imm.13493
Cell Metab, 2018, 28(3):476-489
Neurotox Res, 2015, 27(3):229-45
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.
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.
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).
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.
S6639 BAY-545 BAY-545 is an A2B adenosine receptor antagonist with ic50 of 59 nM.
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.
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00163-1
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.
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 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
Nat Commun, 2021, 12(1):4789
Nat Methods, 2020, 17(3):279-282
J Cell Physiol, 2020, 235(3):2441-2451
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.
J Neurochem, 2021, 10.1111/jnc.15436
Neurochem Int, 2021, 145:104983
Haematologica, 2020, 16 pii: haematol
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
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.
Mol Cancer Res, 2019, 17(5):1166-1179
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
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.
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.
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.
Cancer Res, 2022, canres.1707.2021
Immunology, 2022, 10.1111/imm.13493
Cancer Lett, 2021, 522:80-92
S2153 CGS 21680 HCl CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
J Neurochem, 2021, 10.1111/jnc.15436
Biomed Res Int, 2020, 2020:2603873
PPAR Res, 2020, 2020:2410264
S5358 Regadenoson Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
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.
E0356New MIPS521

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

S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) 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 S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) S-(4-Nitrobenzyl)-6-thioinosine (NBMPR, Nitrobenzylthioinosine, NBTI, NSC 296962) is an inhibitor of ENT1 transporter that crosses the blood-brain barrier and is able to potentiate the neuroprotective effects of adenosine.
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.
S2790 Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.
Immunology, 2022, 10.1111/imm.13493
Cell Metab, 2018, 28(3):476-489
Neurotox Res, 2015, 27(3):229-45
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.
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.
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).
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.
S6639 BAY-545 BAY-545 is an A2B adenosine receptor antagonist with ic50 of 59 nM.
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.
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00163-1
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.
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 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
Nat Commun, 2021, 12(1):4789
Nat Methods, 2020, 17(3):279-282
J Cell Physiol, 2020, 235(3):2441-2451
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.
J Neurochem, 2021, 10.1111/jnc.15436
Neurochem Int, 2021, 145:104983
Haematologica, 2020, 16 pii: haematol
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
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.
Mol Cancer Res, 2019, 17(5):1166-1179
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
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.
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.
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.
Cancer Res, 2022, canres.1707.2021
Immunology, 2022, 10.1111/imm.13493
Cancer Lett, 2021, 522:80-92
S2153 CGS 21680 HCl CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
J Neurochem, 2021, 10.1111/jnc.15436
Biomed Res Int, 2020, 2020:2603873
PPAR Res, 2020, 2020:2410264
S5358 Regadenoson Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
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.
E0356New MIPS521

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

E0356New MIPS521

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

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