S82581 |
Fatostatin A |
源葉(MedMol) | 99% |
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- 產(chǎn)品描述: Fatostatin (125B11) 是一種diarylthiazole的衍生物,是 Sterol regulatory element binding proteins (SREBPs) 活化的特異性抑制劑。Fatostatin 可結(jié)合SCAP (SREBP cleavage-activating protein),并抑制SREBP的ER-Golgi易位。Fatostatin 可抑制癌細胞生長并增強癌細胞的凋亡
- 靶點: SREBP;NPC1L1;?FattyAcidSynthase
- 體外研究:
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
- 體內(nèi)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
- 細胞實驗: 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.
- 動物實驗: Animal Models: 4-to-5-week-old homozygous male obese (ob/ob) mice (C57BL/6J) Dosages: 30 mg/kg Administration: IP
- 參考文獻:
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
- 保存條件: -20℃
- 配置溶液濃度參考:
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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質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)