Adenosine Receptor

Inhibitory Selectivity

Adenosine Receptor Products

All (23) Adenosine Receptor Inhibitors (2) Adenosine Receptor Antagonists (15) Adenosine Receptor Agonists (6)

Catalog No.	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.
S2790	Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with K_i of 2.2 nM. Phase 3.	Cell Metab, 2018, 28(3):476-489 Neurotox Res, 2015, 27(3):229-45	The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)
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
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).
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.
S8105	ZM241385 ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.	Cell Mol Immunol, 2020, 10 Biomed Res Int, 2020, 2020:2603873 Oxid Med Cell Longev, 2020, 2020:7649080	T cells treated with MTX, astilbin, ZM241385 and SCH772984. The levels of p-ERK1/2, p-P65, p-STAT1 and p-STAT3 were analyzed by western blot.
S6639	BAY-545 BAY-545 is an A_2B 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 A_2A 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.
S8104	SCH58261 SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i 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
S7588	Reversine Reversine is a potent human A3 adenosine receptor antagonist with K_i 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	Immunofluorescence of acetylated a-tubulin (red) in control (a), reversin-treated (b), and BI 2536/Reversin mixture-treated embryos (c).The embryos treated with Reversine completed first mitosis, but the nuclei of their blastomeres were fragmented (b, arrows). Embryos inhibited withthe BI 2536/Reversine mixture arrested before the onset of anaphase. Microtubules of the spindle are disorganized (c, double-arrow) and thechromosomes are misaligned (c, arrows) in these inhibited embryos. DNA is counter-stained with DAPI (blue). Scale bar, 10 μm.
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.
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
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.	J Neurochem, 2021, 10.1111/jnc.15436 Biomed Res Int, 2020, 2020:2603873 PPAR Res, 2020, 2020:2410264	Effects of CGS-21,680 and forskolin on caffeine inhibited the expression of leptin in the human BeWo cells. The cells were treated with CGS-21,680 (2 μM, adenosine receptor A2a (ADORA2A) agonist)/forskolin (4 μM, adenylyl cyclase (AC) agonist, cAMP activator) and/or caffeine (20 μM) for 7 d. (A and B) The mRNA expression of leptin and ADORA2A was detected by quantitative real-time PCR, n = 3. (C) The protein expression of ADORA2A was detected by Western blotting, n = 2. (D) At the end of the treatment, the mRNA expression of leptin was detected by real-time PCR, n = 3. GAPDH was used as an internal control. The results are expressed as the mean ± S.E.M. of three independent experiments; P < 0.05 and *P < 0.01 vs. control.
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 Lett, 2021, 522:80-92 Front Cell Neurosci, 2018, 12:139 ACS Appl Mater Interfaces, 2016, 8(39):25818-25824
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.
S6347^New	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.
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.

Catalog No.

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.

Catalog No.	Information	Product Use Citations	Product Validations
S2790	Istradefylline Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with K_i of 2.2 nM. Phase 3.	Cell Metab, 2018, 28(3):476-489 Neurotox Res, 2015, 27(3):229-45	The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)
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
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).
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.
S8105	ZM241385 ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.	Cell Mol Immunol, 2020, 10 Biomed Res Int, 2020, 2020:2603873 Oxid Med Cell Longev, 2020, 2020:7649080	T cells treated with MTX, astilbin, ZM241385 and SCH772984. The levels of p-ERK1/2, p-P65, p-STAT1 and p-STAT3 were analyzed by western blot.
S6639	BAY-545 BAY-545 is an A_2B 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 A_2A 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.
S8104	SCH58261 SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i 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
S7588	Reversine Reversine is a potent human A3 adenosine receptor antagonist with K_i 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	Immunofluorescence of acetylated a-tubulin (red) in control (a), reversin-treated (b), and BI 2536/Reversin mixture-treated embryos (c).The embryos treated with Reversine completed first mitosis, but the nuclei of their blastomeres were fragmented (b, arrows). Embryos inhibited withthe BI 2536/Reversine mixture arrested before the onset of anaphase. Microtubules of the spindle are disorganized (c, double-arrow) and thechromosomes are misaligned (c, arrows) in these inhibited embryos. DNA is counter-stained with DAPI (blue). Scale bar, 10 μm.
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.
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
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.

Catalog No.	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.	J Neurochem, 2021, 10.1111/jnc.15436 Biomed Res Int, 2020, 2020:2603873 PPAR Res, 2020, 2020:2410264	Effects of CGS-21,680 and forskolin on caffeine inhibited the expression of leptin in the human BeWo cells. The cells were treated with CGS-21,680 (2 μM, adenosine receptor A2a (ADORA2A) agonist)/forskolin (4 μM, adenylyl cyclase (AC) agonist, cAMP activator) and/or caffeine (20 μM) for 7 d. (A and B) The mRNA expression of leptin and ADORA2A was detected by quantitative real-time PCR, n = 3. (C) The protein expression of ADORA2A was detected by Western blotting, n = 2. (D) At the end of the treatment, the mRNA expression of leptin was detected by real-time PCR, n = 3. GAPDH was used as an internal control. The results are expressed as the mean ± S.E.M. of three independent experiments; P < 0.05 and *P < 0.01 vs. control.
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 Lett, 2021, 522:80-92 Front Cell Neurosci, 2018, 12:139 ACS Appl Mater Interfaces, 2016, 8(39):25818-25824
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.
S6347^New	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.
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.

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Inhibitory Selectivity

Adenosine Receptor Products