FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.
Treatment of the CHO-K1 cells with analog FGH10019 decreases the percentage of the mature form of SREBP-2 (68 kDa) at lower concentrations than treatment with fatostatin. Densitometric analysis of the gels indicates that the IC50 of analog FGH10019 is approximately 1 μM, which is 5-10 times lower than the IC50 of fatostatin (appr 10 μM)[1].
FGH10019-treated chow is fed at a dose rate calculated to provide about 0.7 mg analog FGH10019 per day, at about 23 mg/kg body weight, to 5-wk-old male ob/ob mice weighing an average of appr 30 g. After 8 wk on the analog 24-treated chow, the mice gain 8-9 % less weight than control mice[1].
[1]. Kamisuki S, et al. Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. J Med Chem. 2011 Jul 14;54(13):4923-7.