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.
|
-
Nat Commun, 2023, 14(1):3364
-
Commun Biol, 2023, 6(1):1271
-
Heliyon, 2023, 9(9):e20182
|
|
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. |
-
Nat Commun, 2022, 13(1):5845
-
Cancer Res, 2022, canres.1707.2021
-
Immunology, 2022, 10.1111/imm.13493
|
|
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 aminophylline (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 是天然的细胞分裂素中最活跃和最普遍的形式,可促进细胞分裂,刺激芽增殖,抑制根形成,减缓衰老过程并激活基因表达和代谢活性。Zeatin Riboside 通过激动哺乳动物的 adenosine A2A receptor 起到免疫调节作用。 |
|
|
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. |
|
|
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. |
-
Nat Commun, 2022, 13(1):5845
-
Cancer Res, 2022, canres.1707.2021
-
Immunology, 2022, 10.1111/imm.13493
|
|
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 aminophylline (AMPH)-induced seizures. |
|
|
S5678 |
trans-Zeatin-riboside
|
Zeatin Riboside 是天然的细胞分裂素中最活跃和最普遍的形式,可促进细胞分裂,刺激芽增殖,抑制根形成,减缓衰老过程并激活基因表达和代谢活性。Zeatin Riboside 通过激动哺乳动物的 adenosine A2A receptor 起到免疫调节作用。 |
|
|
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. |
|
|
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 Commun, 2023, 14(1):3364
- Commun Biol, 2023, 6(1):1271
- Heliyon, 2023, 9(9):e20182
|
|
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. |
- Nat Commun, 2022, 13(1):5845
- Cancer Res, 2022, canres.1707.2021
- Immunology, 2022, 10.1111/imm.13493
|
|
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 aminophylline (AMPH)-induced seizures. |
|
|
S5678 |
trans-Zeatin-riboside
|
Zeatin Riboside 是天然的细胞分裂素中最活跃和最普遍的形式,可促进细胞分裂,刺激芽增殖,抑制根形成,减缓衰老过程并激活基因表达和代谢活性。Zeatin Riboside 通过激动哺乳动物的 adenosine A2A receptor 起到免疫调节作用。 |
|
|
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. |
|
|