A2AAR antagonist 5
A2AAR antagonist 5 is a selective A2AAR antagonist. A2AAR antagonist 5 inhibits NECA-stimulated adenylyl cyclase activity in hA2AAR-expressing CHO cells with an IC50 value of 1863 nM. A2AAR antagonist 5 possesses strong free radical scavenging activity, with an EC50 value of 22.21 μM in the DPPH assay. A2AAR antagonist 5 exerts notable neuroprotective effects in in vitro cerebral ischemia models. A2AAR antagonist 5 can be used for the study of cerebral ischemia.
For research use only. We do not sell to patients.
- Formula: C23H20N8O3
- Molecular Weight:456.46
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adenosine Receptor Isoforms
More
Biological Activity
|
hA2AAR 1863 nM (IC50) |
hA2AAR 57 nM (Ki) |
hA1AR > 30000 nM (Ki) |
hA3 358 nM (Ki) |
hA2B > 30000 nM (Ki) |
A2AAR antagonist 5 (Compound 3) exhibits potent affinity for hA2A adenosine receptor with a Ki value of 57 nM, shows no affinity for hA1 adenosine receptor (Ki > 30,000 nM), has moderate affinity for hA3 adenosine receptor (Ki = 358 nM), and no activity on hA2B adenosine receptor (IC50 > 30,000 nM)[1].
A2AAR antagonist 5 exerts antagonistic activity against hA2A adenosine receptor in CHO cells expressing hA2A , with an IC50 value of 1416 nM for inhibiting NECA-stimulated adenylyl cyclase activity[1].
A2AAR antagonist 5 displays potent free radical scavenging activity, with an EC50 value of 22.21 μM[1].
A2AAR antagonist 5 (200 nM, administered 15 min before, during Oxygen-Glucose Deprivation (OGD), and 5 min after OGD significantly delays the onset of anoxic depolarization (AD) induced by oxygen-glucose deprivation (OGD) in the CA1 region tested in acute rat hippocampal slices[1].
A2AAR antagonist 5 (1-10 μM, administered during 30 min OGD and subsequent 24 h recovery) exerts significant neuroprotective effects, reducing OGD-induced neuronal damage in the CA1 subfield tested in rat organotypic hippocampal slices [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
Molecular Weight 456.46
-
Formula C23H20N8O3
-
SMILES
O=C(NC1=CC=C(C2=CN3C(C(N)=N2)=NN(C4=CC=CC=C4)C3=O)C=C1)CN5N=C(C)CC5=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)