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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-MK-1088
MK-1088

Chemical Structure : MK-1088

CAS No.: 2433765-51-4

MK-1088 (MK1088)

货号: PC-26707Not For Human Use, Lab Use Only.

MK-1088 is a potent, selective dual adenosine A2A receptor (A2AR) and A2B receptor (A2BR) antagonist with Ki values of 0.31 nM and 5.3 nM for human A2AR and A2BR respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MK-1088 is a potent, selective dual adenosine A2A receptor (A2AR) and A2B receptor (A2BR) antagonist with Ki values of 0.31 nM and 5.3 nM for human A2AR and A2BR respectively.
MK-1088 displays >100-fold selectivity over A1R and A3R versus A2AR.
MK-1088 exhibits high affinity for mouse A2AR and A2BR with Ki of 3.2 nM and 28 nM respectively.
MK-1088 shows potential to reverse adenosine-mediated suppression of tumor immune surveillance as either a single-agent treatment or in combination with other immunotherapy agents such as anti-PD-1/PD-L1 monoclonal antibodies.

物理化学性质&存储条件

分子量 468.54
分子式 C23H29FN8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(4-((2S,5R)-5-(5-Amino-9-fluoro-8-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-2-yl)-2-methylpiperidin-1-yl)-1H-pyrazol-1-yl)-2-methylpropan-2-ol

参考文献

1. Zhang Y, et al. J Med Chem. 2026 May 5. doi: 10.1021/acs.jmedchem.5c03405.

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