MAP4K4-IN-3 (Compound 17) 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. Antidiabetic agent.
体外研究
MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic agents.
体内研究
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. Substantial weight losses (7%) and body temperature increases (0.4°C) relative to controls are observed over the course of the study. For cardiovascular end points, maximal heart rate increases of 25 bpm, relative to controls, are induced by treatment with MAP4K4-IN-3.
分子式
C15H12ClN5
分子量
297.74
CAS号
1811510-58-3
运输条件
Room temperature in continental US; may vary elsewhere.