1. GPCR/G Protein
  2. Adenosine Receptor
  3. A2AR/A2BR antagonist 2

A2AR/A2BR antagonist 2 is a dual A2A/A2B adenosine receptor antagonist with selectivity for the A1 receptor. A2AR/A2BR antagonist 2 reverses adenosine-mediated T-cell immunosuppression in the tumor microenvironment. A2AR/A2BR antagonist 2 can be used in cancer-related research.

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A2AR/A2BR antagonist 2

A2AR/A2BR antagonist 2 Chemical Structure

CAS No. : 2975718-45-5

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Description

A2AR/A2BR antagonist 2 is a dual A2A/A2B adenosine receptor antagonist with selectivity for the A1 receptor. A2AR/A2BR antagonist 2 reverses adenosine-mediated T-cell immunosuppression in the tumor microenvironment. A2AR/A2BR antagonist 2 can be used in cancer-related research[1].

In Vitro

A2AR/A2BR antagonist 2 (compound 34) potently inhibits recombinant A2AR (Ki = 0.3 nM, cAMP IC50 = 4.2 nM) and recombinant A2BR (cAMP IC50 = 21.1 nM), and exhibits high selectivity for recombinant A1R (Ki = 541.0 nM) with a selectivity factor of approximately 1803-fold[1].
A2AR/A2BR antagonist 2 exhibits off-target inhibitory activity against protein serine/threonine kinases (IC50 = 1 μM), as well as off-target inhibitory activity against muscarinic M1-M4 receptors (IC50 = 2-6 μM), serotonin 5-HT1B receptor (IC50 = 2 μM) and 5-HT2B receptor (IC50 = 5 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

418.49

Formula

C22H26N8O

CAS No.
SMILES

COC1=CC=CC2=C1N=C(N3N=C(N=C23)[C@H]4C[C@@H](C4)C5=C(N=C(C=N5)C(C)(N)C)C)N

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  • 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.

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A2AR/A2BR antagonist 2
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HY-183239
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