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

A2AR-antagonist-1 (compound 38) 是一种口服有效的腺苷 A2A 受体 (A2AR) 拮抗剂 (IC50=29 nM)。A2AR-antagonist-1 具有抗肿瘤活性和小鼠肝微粒体代谢稳定性 (t1/2=86.1 min)。A2AR-antagonist-1 也是一种 T 细胞激活剂，通过抑制免疫抑制分子 (LAG-3 和 TIM-3) 和增强效应分子 (GZMB、IFNG 和 IL-2)。

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A2AR-antagonist-1 Chemical Structure

A2AR-antagonist-1 Chemical Structure

CAS No. : 2922920-71-4

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A2AR-antagonist-1 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

A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2)[1].

IC50 & Target[1]

A2AR

29 nM (IC50)

体外研究
(In Vitro)

A2AR-antagonist-1（0.001-10 μM；30 分钟）降低 HEK293-A2AR 细胞中 NECA 诱导的磷酸化 ERK 水平[1]。
A2AR-antagonist-1（0.1-10 μM；5 小时）抑制 NECA 诱导的免疫分子表达并增加 Jurkat T 细胞（人永生化 T 淋巴细胞系）[1] 中的效应分子表达。< br/> A2AR-antagonist-1（0.1-10 μM; 48 h）恢复 OT-I 小鼠脾细胞 (OT-I CTL) 对 MC38-OVA 细胞的细胞毒功能损伤，增强体外 T 细胞的活化和效应功能[1]。

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

A2AR-antagonist-1 相关抗体:

RT-PCR[1]

Cell Line: Jurkat T cells
Concentration: 0.1 μM, 1 μM, and 10 μM
Incubation Time: 5 hours
Result: Reversed NECA (1 μM)-induced up-regulation of immunosuppressive molecules (LAG-3 and TIM-3), and NECA-induced down-regulation of effector molecules (GZMB, IFNG, and IL-2).

Immunofluorescence[1]

Cell Line: Cytotoxic T lymphocytes from OT-I mouse splenocyte (OT-I CTL)
Concentration: 0.1 μM, 1 μM, and 10 μM
Incubation Time: 48 hours
Result: Increased relative killing ability of OT-I CTL according to image.
体内研究
(In Vivo)

A2AR-antagonist-1（100 mg/kg；口服；每天一次，持续 23 天）在携带结肠癌 MC38 细胞的 C57BL/6 小鼠体内表现出优异的抗肿瘤活性[1]。

在小鼠中的药代动力学分析[1]

Route Dose (mg/kg) Cmax (ng/mL) AUC0-last (ng·h/mL) AUC0-t (ng·h/mL) t1/2 (h) F (%)
i.v. 2 2584 5577 5565 0.93 /
p.o. 10 8823 24008 24003 2.35 86.1

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

Animal Model: MC38 xenograft model in mouse[1]
Dosage: 100 mg/kg
Administration: PO; once daily for 23 days
Result: Promoted CD8+ T cell accumulation.
Enhanced antitumor immunity, promoted tumor regression.
Had insignificant effect on body weight of the mice.
分子量

451.52

Formula

C27H25N5O2
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

A2AR-antagonist-1 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:

A2AR-antagonist-12922920-71-4Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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