FGH10019

• CAT Number: I000255
• CAS Number: 1046045-61-7
• Molecular Formula: C18H19N3O2S2
• Molecular Weight: 373.49
• Purity: ≥95%
• Synonyms: N-[4-[2-(2-propylpyridin-4-yl)-1,3-thiazol-4-yl]phenyl]methanesulfonamide
• InChI: InChI=1S/C18H19N3O2S2/c1-3-4-16-11-14(9-10-19-16)18-20-17(12-24-18)13-5-7-15(8-6-13)21-25(2,22)23/h5-12,21H,3-4H2,1-2H3
• InChIKey: OWAXXHRQPWGNTG-UHFFFAOYSA-N
• SMILES: CCCC1=NC=CC(=C1)C2=NC(=CS2)C3=CC=C(C=C3)NS(=O)(=O)C

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].

Reference

[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.
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