MAP4K4-IN-3 是MAP4K4选择性抑制剂,在激酶实验中IC50为 14.9 nM,在细胞实验中IC50为 470 nM。具有抗糖尿病作用。
产品描述
MAP4K4-IN-3 may be a viable target for antidiabetic agents, a serine/threonine protein kinase.
体外活性
MAP4K4-IN-3, Antidiabetic agent.MAP4K4-IN-3 is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay.
体内活性
Oral dosing in telemetered rats for 5 days with MAP4K4-IN-3 (Compound 2;?25 mg/kg, b.i.d.) results in a number of adverse effects.For cardiovascular end points, maximal heart rate increases of 25 bpm, relative to controls, are induced by treatment with MAP4K4-IN-3[2].?Substantial weight losses (7%) and body temperature increases (0.4°C) relative to controls are observed over the course of the study.?
Cas No.
1811510-58-3
分子式
C15H12ClN5
分子量
297.74
别名
Compound 17
储存和溶解度
DMSO:8 mg/mL (26.87mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years