货号:A1193404 同义名: AB928;A2aR/A2bR antagonist-1
AB928 is a dual A2aR/A2bR antagonist that inhibits A2aR and A2bR with an equilibrium binding constant of 1.4 and 2 nM, respectively.
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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产品名称 | Adenosine Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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ZM241385 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Istradefylline |
+++
Adenosine A2A receptor, Ki: 2.2 nM |
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Reversine |
+
human A3 adenosine receptor, Ki: 0.66 μM |
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SCH58261 |
++++
bovine A2a, Ki: 2.0 nM rat A2a, Ki: 2.3 nM |
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A2A receptor antagonist 1 |
++
A1R, Ki: 264 nM A2AR, Ki: 4 nM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Adenosine is an endogenous modulator that triggers multiple signaling pathways through four G-protein-coupled adenosine receptors A1R, A2aR, A2bR, and A3R. A2aR and A2bR are the receptors that primarily expressly in immune cells (T cells and myeloid cells, respectively). AB928 is a dual A2aR/A2bR antagonist that inhibits A2aR and A2bR with an equilibrium binding constant of 1.4 and 2 nM, respectively[1]. In the presence of adenosine, human monocyte-derived dendritic cells differentiated and exhibited a reduced ability to stimulate IFN-γ secretion from allogenic CD4+ T-cells in a mixed lymphocyte reaction. However, the addition of AB928 reversed adenosine-mediated suppression of dendritic cell function. AB928 also rescued gene expressions regulated by adenosine during the differentiation of human monocyte-derived dendritic cells[2]. In human whole blood, AB928 at 90 nM inhibited 50% of the 5 μM 5'-N-Ethylcarboxamidoadenosine-induced phosphorylation of cAMP response element-binding protein[3]. In C57BL/6 mice inoculated with mouse mammary tumor AT3-OVA, the concurrent treatment with AB928 and chemotherapy resulted in a significant reduction in tumor volume as compared to chemotherapy alone (28 mg vs. 86 mg). Also, mice treated with both AB928 and chemotherapy exhibited increased immune cell infiltrate and stromal response in tumors. Treatment with AB928 in combination with α-PD-1 therapy also suppressed the growth of melanoma B16-F10 tumors in inoculated mice[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.72mL 2.34mL 1.17mL |
23.45mL 4.69mL 2.34mL |
CAS号 | 2239273-34-6 |
分子式 | C23H22N8O |
分子量 | 426.474 |
别名 | AB928;A2aR/A2bR antagonist-1 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 | |
动物实验配方 |