2. GPCR/G Protein
  3. Adenosine Receptor
  4. 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。

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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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A2A receptor antagonist 2 相关抗体

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查看 Adenosine Receptor 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

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

A2A receptor antagonist 2 相关抗体:

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].

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
分子量

493.53

Formula

C25H28FN7O3
CAS 号
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.
纯度 & 产品资料
参考文献

A2A receptor antagonist 2 相关分类

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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.

Keywords:

A2A receptor antagonist 22767206-20-0Adenosine ReceptorP1 receptorJurkat T cellsHCT116Inhibitorinhibitorinhibit

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产品名称：
A2A receptor antagonist 2
目录号：
HY-144672
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