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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Diglyceride Acyltransferase (DGAT)-PF-07202954
PF-07202954

Chemical Structure : PF-07202954

CAS No.: 2639372-47-5

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PF-07202954 (PF 07202954)

货号: PC-21285Not For Human Use, Lab Use Only.

PF-07202954 is a potent, selective next-generation DGAT2 inhibitor with IC50 of 10 nM (hDGAT2).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PF-07202954 is a potent, selective next-generation DGAT2 inhibitor with IC50 of 10 nM (hDGAT2).
PF-07202954 exhibits rat DGAT2 in vitro potency similar to that of human (IC50=17 nM).
PF-07202954 display high selectivity against related acyltransferases (DGAT1, MGAT1, MGAT2, and MGAT3: all IC50 > 50,000 nM) and a broad off-target panel.
PF-07202954 (3-100 mg/ kg) dose dependenlyly reduces hepatic and circulating triglycerides, along with SREBP target gene expression reduction, in Western-diet-fed rats.

物理化学性质&存储条件

分子量 438.46
分子式 C22H23FN6O3
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

2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-((3S,5S)-5-fluoropiperidin-3-yl)pyrimidine-5-carboxamide

参考文献

1. Kevin J Filipski, et al. ACS Med Chem Lett. 2023 Oct 2;14(10):1427-1433.

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