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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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥7857 有现货
100MG 获取报价 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Ro 48-8071
  • 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
  • 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。
  • 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.
  • 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.
  • 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.
  • 同义词
    Ro-488071
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Other Targets
  • 研究领域
    Cardiovascular Disease
  • 适应症
    Dyslipidemia

化学信息

  • CAS Number
    161582-11-2
  • 分子量
    448.3684
  • 分子式
    C23H27BrFNO2
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    CN(CCCCCCOC1=CC(=C(C=C1)C(=O)C2=CC=C(C=C2)Br)F)CC=C
  • 化学全称
    Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 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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