脂肪抑制素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetFatostatinCat. No.: HY-14452CAS No.: 125256-00-0分式: CHNS分量: 294.41作靶點: Fatty Acid Synthase (FAS)作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 27 mg/mL (91.71 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but sa

2、turation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.3966 mL 16.9831 mL 33.9662 mL5 mM 0.6793 mL 3.3966 mL 6.7932 mL10 mM 0.3397 mL 1.6983 mL 3.3966 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實

3、驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.49 mM); Clear solution此案可獲得 2.5 mg/mL (8.49 mM

4、，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.49 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (8.49 mM) 的均勻懸濁液

5、，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.49 mM); Suspended solution; Need ultrasonic此案可獲得 2.5 mg/mL (8.49 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLO

6、GICAL ACTIVITY物活性 Fatostatin (125B11)是SREBP 活化的特異性抑制劑，可抑制 SREBP-1 和 SREBP-2 的活化。Fatostatin 與 SCAP (SREBP裂解激活蛋) 結(jié)合，抑制 SREBPs 的 ER-Golgi 易位。Fatostatin 降低了細胞中成脂基因的轉(zhuǎn)錄。Fatostatin 具有抗腫瘤作，能降低 ob/ob 的糖。體外研究 Fatostatin (125B11) (0.1-1 M; 3 days) inhibits the androgen-independent prostate cancer cell prolifer

7、ation (IC50=0.1M) in an independent of the known IGF1-signaling pathway. Fatostatin inhibits insulin-induced adipogenesis of 3T3-L1 cells1.Fatostatin directly binds SCAP and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 M in mammalian cells.Cell Proliferation Assay1Cell Line: DU-145 cells

8、Concentration: 0.1, 1 MIncubation Time: 3 daysResult: Impaired the IGF1-induced growth at an IC50 of 0.1 M.體內(nèi)研究 Fatostatin (125B11) (30 mg/kg; 150 mL; i.p. injection; daily for 28 days) reduces adiposity, ameliorated fatty liver byreducing triglyceride (TG) storage, and lowered hyperglycemia in ob/o

9、b mice2.Animal Model: Four-to-five-week-old homozygous male obese (ob/ob) mice (C57BL/6J)2Dosage: 30 mg/kg; 150 mLAdministration: i.p. injection; daily for 28 daysResult: Blocked increases in body weight, blood glucose, and hepatic fat accumulation inobese ob/ob mice, even under uncontrolled food in

10、take.戶使本產(chǎn)品發(fā)表的科研獻 Autophagy. 2020 May 20;1-22. J Exp Clin Cancer Res. 2019 May 29;38(1):228. Oncol Rep. 2018 Apr;39(4):1919-1929.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Li X et al. Fatostatin displays high antitumor activity in prostate

11、 cancer by blocking SREBP-regulated metabolic pathways and androgen receptorsignaling. Mol Cancer Ther. 2014 Apr;13(4):855-66.2. Shao W et al. Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner. J Lipid Res. 2016 Aug;57(8):1564-73.3. Inoue K et al. Fatostatin, an

12、 SREBP inhibitor, prevented RANKL-induced bone loss by suppression of osteoclast differentiation. Biochim Biophys Acta.2015 Nov;1852(11):2432-41.4. Choi Y, et al. Identification of bioactive molecules by adipogenesis profiling of organic compounds. J Biol Chem. 2003 Feb 28;278(9):7320-4.5. Kamisuki S, et al. A small molecule that blocks fat synthesis by inhibiting the activation of SREBP. Chem Biol. 2009 Aug 28;16(8):882-92.McePdfHeightCaution: Product has no