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161582-11-2

中文名稱 RO 48-8071鹽
英文名稱 (4-BROMOPHENYL)[3-FLUORO-4-[[6-(METHYL-2-PROPENYLAMINO)HEXYL]OXY]PHENYL]-METHANONE
CAS 161582-11-2
分子式 C23H27BrFNO2
分子量 448.37
MOL 文件 161582-11-2.mol
更新日期 2024/11/15 18:20:30
161582-11-2 結構式 161582-11-2 結構式

基本信息

中文別名
RO 48-8071鹽
(4-溴苯基)[2-氟-4-[[6-(甲基-2-丙烯基氨基)己基]氧基]苯基]甲酮
英文別名
RO 48-8071
(4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propenylamino)hexyl]oxy]phenyl]methanone
(4-BROMOPHENYL)[3-FLUORO-4-[[6-(METHYL-2-PROPENYLAMINO)HEXYL]OXY]PHENYL]-METHANONE
Methanone, (4-broMophenyl)[2-fluoro-4-[[6-(Methyl-2-propenylaMino)hexyl]oxy]phenyl]-
Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]-
所屬類別
生物化工:激動劑抑制劑

物理化學性質

沸點522.8±50.0 °C(Predicted)
密度1.235±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:2): .25 mg/ml
酸度系數(shù)(pKa)8.88±0.50(Predicted)

常見問題列表

生物活性
Ro 48-8071 是氧化鯊烯環(huán)化酶 (Oxidosqualene cyclase) 抑制劑,IC50 約為 6.5 nM。
靶點

IC50: appr 6.5 nM (Oxidosqualene cyclase)

體外研究

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.

體內(nèi)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.

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