
Ro 48-8071
CAS No. 161582-11-2
Ro 48-8071 ( Ro-488071 )
产品货号. M12352 CAS No. 161582-11-2
一种有效的 2,3-氧化角鲨烯环化酶 (OSC) 抑制剂,IC50 为 6.5 nM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥7857 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Ro 48-8071
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述一种有效的 2,3-氧化角鲨烯环化酶 (OSC) 抑制剂,IC50 为 6.5 nM。
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产品描述A potent 2,3-oxidosqualene cyclase (OSC) inhibitor with IC50 of 6.5 nM; 6 times less potent against hamster and Gottingen minipig liver OSC, and 10-times more potent against squirrel monkey liver OSC; blocks human liver OSC and cholesterol synthesis in HepG2 cells in the nanomolar range; triggers the production of monooxidosqualene, dioxidosqualene, and epoxycholesterol.Dyslipidemia Preclinical.
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体外实验In HepG2 cells, Ro 48-8071 reduces cholesterol synthesis dose dependently with an IC50 value of appr 1.5 nM. Ro 48-8071 (10 μM) significantly reduces the viability of PC-3 prostate cancer cells, but not normal prostate cells. Ro 48-8071 (10-30 μM) induces apoptosis of both LNCaP and C4-2 cell lines in a dose-dependent manner. And castration-resistant PC-3 and DU145 cells also demonstrate significant levels of apoptosis following 24-hour treatment with Ro 48-8071. Ro 48-8071 (10-25 μM) reduces AR protein expression in a dose-dependent manner. Ro 48-8071 (0.1-1 μM) increases ERβ protein expression dose-dependently in both hormone-dependent LNCaP and castration-resistant PC-3 cells. Using mammalian cells engineered to express human ERα or ERβ protein, together with an ER-responsive luciferase promoter, Ro 48-8071 dose-dependently inhibits 17β-estradiol (E2)-induced ERα responsive luciferase activity (IC50, appr 10 μM), under conditions that are non-toxic to the cells.
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体内实验Ro 48-8071 lowers LDL-C maximally appr 60% at 150 μmol/kg per day, with no further reduction up to 300 μmol/kg per day, leaving HDL-C unchanged at all doses in hamsters. Ro 48-8071 (≥00 μmol/kg per day) increases the amount of MOS in liver of hamsters. Ro 48-8071 (300 μmol/kg per day) remarkedly and significantly reduces VLDL secretion of hamsters. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Furthermore, Ro 48-8071 at a concentration of 20 mg/kg, completely eradicates two of the 12 tumors being monitored in the mice in the timeframe tested. Ro 48-8071 (20 mg/day/kg body weight) leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine of BALB/c mice. Sterol synthesis is also reduced in the large intestine and stomach.
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同义词Ro-488071
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通路Others
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靶点Other Targets
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受体Other Targets
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研究领域Cardiovascular Disease
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适应症Dyslipidemia
化学信息
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CAS Number161582-11-2
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分子量448.3684
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分子式C23H27BrFNO2
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCN(CCCCCCOC1=CC(=C(C=C1)C(=O)C2=CC=C(C=C2)Br)F)CC=C
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化学全称Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Morand OH, et al. J Lipid Res. 1997 Feb;38(2):373-90.
2. Peffley DM, et al. Biochem Pharmacol. 1998 Aug 15;56(4):439-49.
3. Liang Y, et al. Onco Targets Ther. 2016 May 30;9:3223-32.
产品手册




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