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PF-06260933
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-06260933图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PF-06260933是一种高度选择性的MAP4K4小分子抑制剂,在激酶实验和细胞实验中的IC50值分别为3.7和160nM。

Cell experiment:

HUVECs are maintained in EGM2 media at 37℃ and 5% CO2. HUVECs or peritoneal macrophages are treated with vehicle or PF-06260933 in vitro to determine whether pharmacological inhibition of MAP4K4 alteres MAPK signalling in response to TNF-α[2].

Animal experiment:

Compound PF-06260933 (10 mg/kg, dissolved in dH2O) is orally administered to 8 to 10-week-old male Apoe-/- mice twice daily for 6 weeks. Ldlr-/- male mice are placed on high-fat diet (HFD) for 10 weeks before drug administration. Compound PF-06260933 is administered to male 8 to 10-week-old Ldlr-/- mice as above for 10 weeks. Oral administration of water is used as vehicle control in all studies. Mice are euthanized by CO2 inhalation followed by bilateral pneumothorax[2].

产品描述

PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.

PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro, similar to MAP4K4 knockdown[2].

In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed[2].

[1]. Ammirati M, et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. [2]. Roth Flach RJ, et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995.