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GPCR/G Protein Adenosine Receptor

Adenosine Receptor

The adenosine receptors are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a different gene.
Cat No. product name
T9238 KI-7 KI-7 is an adenosine A2B receptor positive allosteric modulator.
T1825 Reversine Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A/B/C(IC50s=150-500 nM).
T7188 Piclidenoson Piclidenoson, a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.
T7183 CPI-444 CPI-444 is an antagonist of the adenosine A2A receptor.It reduces tumor area in mouse model of murine Her2/neu-expressing breast cancer.
T6884 2-Cl-IB-MECA 2-Cl-IB-MECA is an adenosine A3 receptor agonist.
T4290 Preladenant Preladenant is an orally bioavailable antagonist of the adenosine A2A receptor (Ki: 1.1 nM) and has >1000-fold selectivity over all other adenosine receptors.
T4265 AZD4635 AZD4635 is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).
T6115 Fostamatinib Fostamatinib(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
T2205 Theophylline-7-acetic acid Theophylline-7-acetic acid, a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the...
T7509 PD 117519 PD 117519 is an agonist of adenosine receptor
T0070 Pentoxifylline Pentoxifylline modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase a...
T2373 Vipadenant Vipadenant(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).
T2671 Regadenoson Regadenoson is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selecti...
T6979 SCH58261 SCH 58261 is a potent and selective A2a adenosine receptor antagonist.The Ki =2.3 nM for rat A2a and 2 nM is for bovine A2a.
T6552 Istradefylline Istradefylline(Ki of 2.2 nM) is a selective adenosine A2A receptor (A2AR) antagonist, which is under development in Phase 3 trails. It has been used in trials st...
T7021 ZM241385 ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.
T7320 Tozadenant Tozadenant is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)
T7683 Adenosine amine congener Adenosine amine congener (ADAC) is an agonist of selective A1 adenosine receptor,.
T23347 SDZ WAG 994 A1 adenosine receptor agonist
T16281 Nelonicline Nelonicline is a selective agonist of neuronal nicotinic receptors.
T23336 SCH 442416 SCH-442416 is an selective antagonist of adenosine A2A receptor. SCH-442416 binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5...
T22744 DPCPX DPCPX is an A1 adenosine receptor antagonist
T8613 1-Ethyl-6-aminouracil 1-Ethyl-6-aminouracil is an intermediate in the synthesis of a series of new substituted Xanthines which have high affinity and selectivity for the human adenosi...
T8598 CHEMBL241987 CHEMBL241987 targets the Adenosine receptor A3 (human)
T17023 Tecadenoson Tecadenoson is a selective agonist of A1 adenosine receptor.
T16378 Ogerin Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83). Ogerin blocks recall in fear conditioning in mice. Ogerin displays inverse agonist and a...
T16158 PF-02575799 PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).
TQ0125 Capadenoson Capadenoson is a selective adenosine-A1 receptor agonist.
T16136 MRS-1706 MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B ...
T11762 Kira8 Hydrochloride Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
T13008 ST3932 ST3932 is a ST1535 metabolite, is a adenosine A2A receptor antagonist(Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively).
T14078 AB928 AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. It has immunomodulatory activity[1].
T8512 BAY-545 BAY-545 is an antagonist of A2B adenosine receptor(IC50 : 59 nM).
T8312 Derenofylline Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)
TQ0136 GR 79236 GR79236 is an effective and selective adenosine A1 receptor agonist (Ki: 3.1 nM) that has analgesic and anti-inflammatory actions.
T6441 CGS 21680 HCl CGS 21680 HCl( IC50=22 nM), an adenosine receptor agonist, exhibits 140-fold potency in A2 receptor over A1 receptor.
KI-7
T9238CAS 1489263-00-4
KI-7 is an adenosine A2B receptor positive allosteric modulator.
Reversine
T1825CAS 656820-32-5
Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A/B/C(IC50s=150-500 nM).
Piclidenoson
T7188CAS 152918-18-8
Piclidenoson, a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.
CPI-444
T7183CAS 1202402-40-1
CPI-444 is an antagonist of the adenosine A2A receptor.It reduces tumor area in mouse model of murine Her2/neu-expressing breast cancer.
2-Cl-IB-MECA
T6884CAS 163042-96-4
2-Cl-IB-MECA is an adenosine A3 receptor agonist.
Preladenant
T4290CAS 377727-87-2
Preladenant is an orally bioavailable antagonist of the adenosine A2A receptor (Ki: 1.1 nM) and has >1000-fold selectivity over all other adenosine receptors.
AZD4635
T4265CAS 1321514-06-0
AZD4635 is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).
Fostamatinib
T6115CAS 901119-35-5
Fostamatinib(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
Theophylline-7-acetic acid
T2205CAS 652-37-9
Theophylline-7-acetic acid, a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the...
PD 117519
T7509CAS 96392-15-3
PD 117519 is an agonist of adenosine receptor
Pentoxifylline
T0070CAS 6493-05-6
Pentoxifylline modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase a...
Vipadenant
T2373CAS 442908-10-3
Vipadenant(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).
Regadenoson
T2671CAS 313348-27-5
Regadenoson is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selecti...
SCH58261
T6979CAS 160098-96-4
SCH 58261 is a potent and selective A2a adenosine receptor antagonist.The Ki =2.3 nM for rat A2a and 2 nM is for bovine A2a.
Istradefylline
T6552CAS 155270-99-8
Istradefylline(Ki of 2.2 nM) is a selective adenosine A2A receptor (A2AR) antagonist, which is under development in Phase 3 trails. It has been used in trials st...
ZM241385
T7021CAS 139180-30-6
ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.
Tozadenant
T7320CAS 870070-55-6
Tozadenant is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)
Adenosine amine congener
T7683CAS 96760-69-9
Adenosine amine congener (ADAC) is an agonist of selective A1 adenosine receptor,.
SDZ WAG 994
T23347CAS 130714-47-5
A1 adenosine receptor agonist
Nelonicline
T16281CAS 1026134-63-3
Nelonicline is a selective agonist of neuronal nicotinic receptors.
SCH 442416
T23336CAS 316173-57-6
SCH-442416 is an selective antagonist of adenosine A2A receptor. SCH-442416 binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5...
DPCPX
T22744CAS 102146-07-6
DPCPX is an A1 adenosine receptor antagonist
1-Ethyl-6-aminouracil
T8613CAS 41862-09-3
1-Ethyl-6-aminouracil is an intermediate in the synthesis of a series of new substituted Xanthines which have high affinity and selectivity for the human adenosi...
CHEMBL241987
T8598CAS 109740-09-2
CHEMBL241987 targets the Adenosine receptor A3 (human)
Tecadenoson
T17023CAS 204512-90-3
Tecadenoson is a selective agonist of A1 adenosine receptor.
Ogerin
T16378CAS 1309198-71-7
Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83). Ogerin blocks recall in fear conditioning in mice. Ogerin displays inverse agonist and a...
PF-02575799
T16158CAS 863491-70-7
PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).
Capadenoson
TQ0125CAS 544417-40-5
Capadenoson is a selective adenosine-A1 receptor agonist.
MRS-1706
T16136CAS 264622-53-9
MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B ...
Kira8 Hydrochloride
T11762CAS 2250019-92-0
Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
ST3932
T13008CAS 1246018-21-2
ST3932 is a ST1535 metabolite, is a adenosine A2A receptor antagonist(Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively).
AB928
T14078CAS 2239273-34-6
AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. It has immunomodulatory activity[1].
BAY-545
T8512CAS 1699717-32-2
BAY-545 is an antagonist of A2B adenosine receptor(IC50 : 59 nM).
Derenofylline
T8312CAS 251945-92-3
Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)
GR 79236
TQ0136CAS 124555-18-6
GR79236 is an effective and selective adenosine A1 receptor agonist (Ki: 3.1 nM) that has analgesic and anti-inflammatory actions.
CGS 21680 HCl
T6441CAS 124431-80-7
CGS 21680 HCl( IC50=22 nM), an adenosine receptor agonist, exhibits 140-fold potency in A2 receptor over A1 receptor.