上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
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 Chemical Structure
| 规格 |
|
是否有货 |
|
| 100 mg |
|
询价 |
|
| 250 mg |
|
询价 |
|
| 500 mg |
|
询价 |
|
* Please select Quantity before adding items.
| 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 |
|
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 |
|
| Formula |
|
| 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.
|
所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务
