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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Diglyceride Acyltransferase (DGAT)-PF-06865571
PF-06865571

Chemical Structure : PF-06865571

CAS No.: 2186700-33-2

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PF-06865571 (Ervogastat, PF 06865571)

货号: PC-72624Not For Human Use, Lab Use Only.

PF-06865571 (Ervogastat, PF 06865571) is a potent, selective diacylglycerol acyltransferase DGAT2 inhibitor with IC50 of 17.2 and 833 nM for human and rat DGAT2, respectively.

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5 mg ￥2280 In stock
10 mg ￥3580 In stock
25 mg ￥5580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-06865571 (Ervogastat, PF 06865571) is a potent, selective diacylglycerol acyltransferase DGAT2 inhibitor with IC50 of 17.2 and 833 nM for human and rat DGAT2, respectively.
PF-06865571 displays no significant inhibitions against MGAT1-3 and DGAT1 (IC50>50 uM).
PF-06865571 showspotent inhibitory activities in human, rat, and monkey hepatocytes with IC50 values of 2.79, 6.02, and 2.13 nM, respectively.
PF-06865571 is a non-time-dependent, reversible, rapid binding inhibitor of DGAT2.
shows no significant inhibitions in hERG, a kinase selectivity panel, and a PDE selectivity panel
PF-06865571 (0.3, 3, 10, 30, or 90 mg/kg, orally twice daily for 7 days) reduces plasma triglyceride levels in sucrose diet-fed Sprague-Dawley rats.

物理化学性质&存储条件

分子量 407.423
分子式 C21H21N5O4
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

5-Pyrimidinecarboxamide, 2-[5-[(3-ethoxy-2-pyridinyl)oxy]-3-pyridinyl]-N-[(3S)-tetrahydro-3-furanyl]-

参考文献

1. Roberto A Calle, et al. Nat Med. 2021 Oct;27(10):1836-1848.
2. Futatsugi K, et al. J Med Chem. 2022 Nov 24;65(22):15000-15013.

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