1. GPCR/G Protein
  2. Adenosine Receptor
  3. A2A receptor antagonist 2

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM.

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A2A receptor antagonist 2 Chemical Structure

A2A receptor antagonist 2 Chemical Structure

CAS No. : 2767206-20-0

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Description

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM[1].

IC50 & Target

A2AR

8.3 nM (IC50)

In Vitro

A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A2AR agonist) [1].
A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells[1].

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

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 10 μM
Incubation Time: Overnight
Result: Increased IL-2 production in the presence of NECA

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 and Jurkat T cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Completely reversed NECA’s suppression of the cytotoxic function of Jurkat T cells.
In Vivo

A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO)[1].

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

Animal Model: C57BL/6 mice[1]
Dosage: 2 or 10 mg/kg
Administration: Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)
Result: PK profiles of A2A receptor antagonist 2 (n = 3)[1]
Parameters
Dosing Route IV (2 mg/kg) PO (10 mg/kg) IP (10mg/kg)
Cmax (ng/mL) 1091 ± 129a 106 ± 33.0 41.8 ± 2.75
AUC0-last (ng/mL*h) 767 ± 107 145 ± 25.9 812 ± 12.0
AUC0-t (ng/mL*h) 764 ± 107 139 ± 25.9 444 ± 13.3
T1/2 (h) 2.05 ± 0.94 2.55 ± 2.39 17.6 ± 0.68
F (%) / 3.78% 11.6%
a This value means C0 = 1091 ± 129 ng/mL
Molecular Weight

493.53

Formula

C25H28FN7O3

CAS No.
SMILES

NC1=NC(C2=CC=C(O2)C)=C3C(N(C(C=N3)=O)CCN4CCN(C[C@@H]4C)C5=CC=C(C=C5F)OC)=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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A2A receptor antagonist 2 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.

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A2A receptor antagonist 2
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HY-144672
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