PF6260933 是一种具有高度选择性及口服有活性的MAP4K4小分子抑制剂,在激酶实验中IC50为 3.7 nM,在细胞实验中IC50为 160 nM。
产品描述
PF-06260933 is a highly selective small-molecule MAP4K4 inhibitor with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
体外活性
PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro.
体内活性
PF-06260933 treatment does not alter plasma lipid content in the mice model, 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.
Cas No.
1811510-56-1
分子式
C16H13ClN4
分子量
296.76
别名
PF6260933;PF 6260933;PF-6260933
储存和溶解度
DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years