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• 产品描述： Fatostatin (125B11) 是一种diarylthiazole的衍生物，是 Sterol regulatory element binding proteins (SREBPs) 活化的特异性抑制剂。Fatostatin 可结合SCAP (SREBP cleavage-activating protein)，并抑制SREBP的ER-Golgi易位。Fatostatin 可抑制癌细胞生长并增强癌细胞的凋亡

• 靶点： SREBP;NPC1L1; FattyAcidSynthase

• 体外研究：
  Fatostatin impairs the activation process of sterol regulatory element binding proteins (SREBPs), thereby decreasing the transcription of lipogenic genes in cells. Fatostatin inhibits the ER-Golgi translocation of SREBPs through binding to their escort protein, the SREBP cleavage-activating protein (SCAP), at a distinct site from the sterol-binding domain

• 体内研究：
  Fatostatin blocks increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice, even under uncontrolled food intake. Fatostatin may serve as a tool for gaining further insights into the regulation of SREBP

• 细胞实验： Cell lines: CHO-K1 cells Concentrations: 20 μM Incubation Time: 20 h Method: CHO-K1 cells are plated out onto a 96-well plate in medium A. The cells are transiently cotransfected with pCMV-PLAP-BP2, pCMV-SCAP, and pAc-b-gal, using Lipofectamine reagent. After incubation for 5 hr, the cells are washed with PBS and then incubated in medium B, in the absence or presence of fatostatin (20 μM) or sterols (10 μg/mL cholesterol and 1 μg/mL 25-hydroxycholesterol). After 20 hr of incubation, an aliquot of the medium is assayed for secreted alkaline phosphatase activity. The cells in each well are lysed and used for measurement of b-galactosidase activities. The alkaline phosphatase activity is normalized by the activity of b-galactosidase.

• 动物实验： Animal Models: 4-to-5-week-old homozygous male obese (ob/ob) mice (C57BL/6J) Dosages: 30 mg/kg Administration: IP

• 参考文献：
  1. Shinji Kamisuki, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92. 2. Shuhong Gao, et al. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma. Oncol Rep. 2018 Apr;39(4):1919-1929.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.397 ml	16.983 ml	33.966 ml
  5 mM	0.679 ml	3.397 ml	6.793 ml
  10 mM	0.34 ml	1.698 ml	3.397 ml
  50 mM	0.068 ml	0.34 ml	0.679 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *