中文名 | Ro 48-8071富马酸盐 |
英文名 | Ro 48-8071 fumarate |
别名 | Ro 48-8071富马酸盐 RO48-8071 富马酸盐 化合物RO 48-8071 FUMARATE (4-((6-(烯丙基(甲基)氨基)己基)氧基)-2-氟苯基)(4-溴苯基)甲酮富马酸盐 (4-溴苯基)[2-氟-4-[[6-(甲基-2-丙烯基氨基)己基]氧基]苯基]甲酮富马酸盐 |
英文别名 | CS-1750 RO48-8071 RO 488071 RO-48-8071 Ro 48-8071 fumarate Ro 48-8071 fumarate salt (4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]methanone (4-((6-(allyl(methyl)amino)hexyl)oxy)-2-fluorophenyl)(4-bromophenyl)methanone fumarate Ro48-8071 |
CAS | 189197-69-1 |
化学式 | C23H27BrFNO2.C4H4O4 |
分子量 | 564.45 |
熔点 | 90-92.7°C |
溶解度 | H2O: 在 ~ 60 °C时> 5mg/ml |
存储条件 | Inert atmosphere,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | white |
体外研究 | In HepG2 cells, Ro 48-8071 reduces cholesterol synthesis dose dependently with an IC 50 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 (IC 50 , appr 10 µM), under conditions that are non-toxic to the cells. |
体内研究 | 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. |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.772 ml | 8.858 ml | 17.717 ml |
5 mM | 0.354 ml | 1.772 ml | 3.543 ml |
10 mM | 0.177 ml | 0.886 ml | 1.772 ml |
5 mM | 0.035 ml | 0.177 ml | 0.354 ml |
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