A2A receptor antagonist 2

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A2A receptor antagonist 2 

A2A receptor antagonist 2 (Compound 57) 是一个有效的、高选择性的 adenosine A2A receptor 拮抗剂， IC50 值为8.3 nM。

A2A receptor antagonist 2

A2A receptor antagonist 2 Chemical Structure

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生物活性

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)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(In Vivo)

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

Shanghai Jinpan Biotech Co Ltd 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

分子量

493.53

Formula

C25H28FN7O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Fazhi Yu, et al. Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8H)-one Derivatives as Novel Potent Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2022 Mar 10;65(5):4367-4386.

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