产品描述: | FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM. |
靶点: |
IC50: 1 μM (SREBP);NPC1L1; FattyAcidSynthase |
体外研究: |
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) |
体内研究: |
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 |
参考文献: |
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. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.677 ml |
13.387 ml |
26.774 ml |
5 mM |
0.535 ml |
2.677 ml |
5.355 ml |
10 mM |
0.268 ml |
1.339 ml |
2.677 ml |
50 mM |
0.054 ml |
0.268 ml |
0.535 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |