A2AAR antagonist 3
A2AAR antagonist 3 is a selective and potent A2A adenosine receptor (A2A AR) antagonist with an IC50 of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A2A AR. A2AAR antagonist 3 demonstrates favorable stability in rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.
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- 화학식: C18H20N8O
- 분자량:364.40
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adenosine Receptor Isoforms
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Biological Activity
A2AAR antagonist 3 (Compound 12a) (1 μM, 48 h) restores NECA-suppressed (1 μM, pretreating for 30 min) IL-2 secretion in human peripheral blood mononuclear cells (PBMCs)[1].
A2AAR antagonist 3 (3.125-100 μM, 24 h) exhibits no significant toxicity towards L929, H9C2, and HTX2426 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L929 (mouse fibroblasts), H9C2 (rat cardiomyocytes), and HTX2426 (human podocytes).
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Concentration:3.125, 6.25, 12.5, 25, 50, and 100 μM
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Incubation Time:24 h
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Result:Exhibited no significant cytotoxicity towards the L929 cells.
Promoted the proliferation of H9C2 cells at concentrations ranging from 3.125 to 25 μM, and showed a slight inhibitory effect at 50 to 100 μM (cell viability 0f 95 %).
Increased cell viability in HTX2426 cells.
Chemical Information
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분자량 364.40
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화학식 C18H20N8O
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SMILES
OC(C)(C)C1=CC=CC(CN2N=NC(C3=NC(N)=NC4=C3C=CN4C)=C2)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)