| Bioactivity | 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]. |
| Invitro | 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。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]。 RT-PCR[1] Cell Line: |
| 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 |
| Name | A2AR-antagonist-1 |
| Formula | C27H25N5O2 |
| Molar Mass | 451.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhu C, et al. Discovery of Pyridinone Derivatives as Potent, Selective, and Orally Bioavailable Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2023 Mar 23. |