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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
T0070 Pentoxifylline Pentoxifylline modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase ...
T1368 Methyl protocatechuate Thermographic recording material with improved image tone.
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).
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 th...
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 select...
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.
T6441 CGS 21680 HCl CGS 21680 HCl( IC50=22 nM),an adenosine receptor agonist, exhibits 140-fold potency in A2 receptor over A1 receptor.
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 s...
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.
T7021 ZM241385 ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.
T4265 AZD4635 AZD4635 is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).
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.
T6884 2-Cl-IB-MECA 2-Cl-IB-MECA is an adenosine A3 receptor agonist.
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.
T7188 Piclidenoson Piclidenoson, a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.
T7320 Tozadenant Tozadenant is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)
T7509 PD 117519 PD 117519 is an agonist of adenosine receptor
T7683 Adenosine amine congener Adenosine amine congener (ADAC) is an agonist of selective A1 adenosine receptor,.
TQ0125 Capadenoson Capadenoson is a selective adenosine-A1 receptor agonist.
TQ0136 GR 79236 GR79236 is an effective and selective adenosine A1 receptor agonist (Ki: 3.1 nM) that has analgesic and anti-inflammatory actions.
T8312 Derenofylline Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)
T14078 AB928 AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. It has immunomodulatory activity[1].
T14944 CGS 15943 CGS 15943 is an orally bioavailable non-xanthine antagonist of Adenosine Receptor. In transfected CHO cells, its Ki for human A1, A2A, A2B, and A3 Adenosine Re...
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).
T11762 Kira8 Hydrochloride Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
T16158 PF-02575799 PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).
T16159 Muramyl dipeptide Muramyl dipeptide is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dip...
T16281 Nelonicline Nelonicline is a selective agonist of neuronal nicotinic receptors.
T8598 CHEMBL241987 CHEMBL241987 targets the Adenosine receptor A3 (human)
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 adenos...
T8512 BAY-545 BAY-545 is an antagonist of A2B adenosine receptor(IC50 : 59 nM).
Pentoxifylline
T0070CAS 6493-05-6
Pentoxifylline modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase ...
Methyl protocatechuate
T1368CAS 2150-43-8
Thermographic recording material with improved image tone.
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).
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 th...
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 select...
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.
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.
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 s...
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.
ZM241385
T7021CAS 139180-30-6
ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.
AZD4635
T4265CAS 1321514-06-0
AZD4635 is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).
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.
2-Cl-IB-MECA
T6884CAS 163042-96-4
2-Cl-IB-MECA is an adenosine A3 receptor agonist.
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.
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.
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)
PD 117519
T7509CAS 96392-15-3
PD 117519 is an agonist of adenosine receptor
Adenosine amine congener
T7683CAS 96760-69-9
Adenosine amine congener (ADAC) is an agonist of selective A1 adenosine receptor,.
Capadenoson
TQ0125CAS 544417-40-5
Capadenoson is a selective adenosine-A1 receptor agonist.
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.
Derenofylline
T8312CAS 251945-92-3
Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)
AB928
T14078CAS 2239273-34-6
AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. It has immunomodulatory activity[1].
CGS 15943
T14944CAS 104615-18-1
CGS 15943 is an orally bioavailable non-xanthine antagonist of Adenosine Receptor. In transfected CHO cells, its Ki for human A1, A2A, A2B, and A3 Adenosine Re...
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).
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.
PF-02575799
T16158CAS 863491-70-7
PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).
Muramyl dipeptide
T16159CAS 53678-77-6
Muramyl dipeptide is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dip...
Nelonicline
T16281CAS 1026134-63-3
Nelonicline is a selective agonist of neuronal nicotinic receptors.
CHEMBL241987
T8598CAS 109740-09-2
CHEMBL241987 targets the Adenosine receptor A3 (human)
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 adenos...
BAY-545
T8512CAS 1699717-32-2
BAY-545 is an antagonist of A2B adenosine receptor(IC50 : 59 nM).