2. GPCR/G Protein
  3. Adenosine Receptor
  4. 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[1].

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A2AAR antagonist 3 Chemical Structure

A2AAR antagonist 3 Chemical Structure

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A2AAR antagonist 3 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

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[1].

In Vitro

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.

A2AAR antagonist 3 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: L929 (mouse fibroblasts), H9C2 (rat cardiomyocytes), and HTX2426 (human podocytes).
Concentration: 3.125, 6.25, 12.5, 25, 50, and 100 μM
Incubation Time: 24 h
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.
Molecular Weight

364.40

Formula

C18H20N8O
SMILES

OC(C)(C)C1=CC=CC(CN2N=NC(C3=NC(N)=NC4=C3C=CN4C)=C2)=N1
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
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A2AAR antagonist 3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A2AAR antagonist 3Adenosine ReceptorP1 receptorA2A adenosine receptorCancerAntagonistInhibitorinhibitorinhibit

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