|3-(2-氨基-6-(1-((6-(2-羟丙基)吡啶-2-基)甲基)-1H-1,2,3-三唑-4-基)嘧啶-4-基)-2-甲基苯腈|CsnPharm

CAS No.: 2239273-34-6

3-(2-Amino-6-(1-((6-(2-hydroxypropan-2-yl)pyridin-2-yl)methyl)-1H-1,2,3-triazol-4-yl)pyrimidin-4-yl)-2-methylbenzonitrile Catalog No. CSN24753

Synonyms: etrumadenant

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

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3448 mL
- 11.7240 mL
- 23.4481 mL
- 5 mM
- 0.4690 mL
- 2.3448 mL
- 4.6896 mL
- 10 mM
- 0.2345 mL
- 1.1724 mL
- 2.3448 mL

技术信息

CAS号

2239273-34-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H22N8O

运输

蓝冰

分子量

426.47

别名

etrumadenant

溶解度

DMSO	67.5 mg/mL (158.3 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

3-(2-Amino-6-(1-((6-(2-hydroxypropan-2-yl)pyridin-2-yl)methyl)-1H-1,2,3-triazol-4-yl)pyrimidin-4-yl)-2-methylbenzonitrile Catalog No. CSN24753

靶点选择性

请登录您的专属账户

确认信息