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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-FM101
FM101

Chemical Structure : FM101

CAS No.: 945457-84-1

FM101 (FM-101, LJ-2698)

货号: PC-23909Not For Human Use, Lab Use Only.

FM101 is a highly potent and selective antagonist of A3 adenosine receptor (A3AR), selectively binds to human A3AR with Ki of 1.44 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FM101 is a highly potent and selective antagonist of A3 adenosine receptor (A3AR), selectively binds to human A3AR with Ki of 1.44 nM.
FM101 causes cAMP inhibition through Gα protein-dependent signaling with EC50 of 104 nM.
FM101 is a potent antagonist of β-arrestin dependent signaling with IC50 of 44 nM.
FM101 induces β-arrestin2-mediated A3AR degradation, leading to mitochondrial dysfunction-mediated necroptosis in Kupffer cells (KCs).
FM101 alleviates MASLD by inducing mitochondrial dysfunction and subsequent necroptosis in monocyte-derived KCs (MoKCs).

物理化学性质&存储条件

分子量 412.29
分子式 C16H15Cl2N5O2S
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

(2R,3R,4S)-2-[2-chloro-6-(3-chlorobenzylamino)-9H purine-9-yl]-tetrahydrothiophene-3,4-diol

参考文献

1. Park JS, et al. Metabolism. 2024 Dec 26;164:156114.

2. Chong-Woo Park, et al. EXCLI J. 2020 Feb 12:19:187-200.

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