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Etrumadenant {[allProObj[0].p_purity_real_show]}

货号:A1193404 同义名: AB928;A2aR/A2bR antagonist-1 Ambeed 开学季,买赠积分,赢豪礼

AB928 is a dual A2aR/A2bR antagonist that inhibits A2aR and A2bR with an equilibrium binding constant of 1.4 and 2 nM, respectively.

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Etrumadenant 化学结构 CAS号:2239273-34-6
Etrumadenant 化学结构
CAS号:2239273-34-6
Etrumadenant 3D分子结构
CAS号:2239273-34-6
Etrumadenant 化学结构 CAS号:2239273-34-6
Etrumadenant 3D分子结构 CAS号:2239273-34-6
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Etrumadenant 纯度/质量文件 产品仅供科研

货号:A1193404 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adenosine Receptor 其他靶点 纯度
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。

Etrumadenant 生物活性

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].

Etrumadenant 参考文献

[1]Seitz L, Jin L, Leleti M, et al. Safety, tolerability, and pharmacology of AB928, a novel dual adenosine receptor antagonist, in a randomized, phase 1 study in healthy volunteers. Invest New Drugs. 2019;37(4):711-721.

[2]AB928, a dual antagonist of the A2aR and A2bR adenosine receptors, relieves adenosine-mediated immune suppression

[3]Pharmacokinetic-pharmacodynamic relationship for AB928, a dual antagonist of the A2aR and A2bR adenosine receptors

Etrumadenant 实验方案

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

Etrumadenant 技术信息

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
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