富马酸盐
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- CAS号:
- 189197-69-1
- 英文名:
- RO 48-8071
- 英文别名:
- CS-1750;Aids163155;Aids-163155;Ro 48-8071 fumarate salt;OSC Inhibitor, Ro 48-8071;RO 488071;RO48-8071;RO-48-8071;OSC Inhibitor, Ro 48-8071 - CAS 189197-69-1 - Calbiochem;Ro 488071 fumarate,Ro 48 8071 fumarate,Ro 48-8071,Inhibitor,inhibit;(4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]methanone;Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propenylamino)hexyl]oxy]phenyl]-,(2E)-2-butenedioate
- 中文名:
- 富马酸盐
- 中文别名:
- RO48-8071 富马酸盐;化合物RO 48-8071 FUMARATE;RO 48-8071,2,3-氧化鲨烯环化酶(OSC)抑制剂;(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
- CBNumber:
- CB9504369
- 分子式:
- C23H27BrFNO2.C4H4O4
- 分子量:
- 564.45
- MOL File:
- 189197-69-1.mol
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富马酸盐化学性质
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熔点:
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90-92.7 °C
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储存条件:
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Inert atmosphere,Store in freezer, under -20°C
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溶解度:
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H2O: >5 mg/mL at ~60 °C
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形态:
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solid
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颜色:
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white
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富马酸盐性质、用途与生产工艺
Ro 48-8071 fumarate 是氧化鲨烯环化酶 (Oxidosqualene cyclase) 抑制剂，IC50 约为 6.5 nM。
IC50: appr 6.5 nM (Oxidosqualene cyclase)
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
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, appr 10 µM), under conditions that are non-toxic to the cells.
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.
富马酸盐
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富马酸盐
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富马酸盐国内生产厂家
189197-69-1, 富马酸盐 相关搜索:
- Inhibitors
- 药靶配体
- 医药
- 小分子抑制剂
- 小分子抑制剂，天然产物
- 抑制剂
- C23H27NO2BrFC4H4O4
- C23H27BrFNO2C4H4O4
- C27H31BrFNO6
- RO 48-8071,2,3-氧化鲨烯环化酶(OSC)抑制剂
- 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
- RO48-8071 富马酸盐
- 189197-69-1
- Ro 488071 fumarate,Ro 48 8071 fumarate,Ro 48-8071,Inhibitor,inhibit
- CS-1750
- RO 488071;RO48-8071;RO-48-8071
- OSC Inhibitor, Ro 48-8071 - CAS 189197-69-1 - Calbiochem
- Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]-, (2E)-2-butenedioate (1:1)
- (4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]methanone
- Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propenylamino)hexyl]oxy]phenyl]-,(2E)-2-butenedioate
- Aids-163155
- Aids163155
- OSC Inhibitor, Ro 48-8071
- (4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]methanone (2E)-2-butenedioate (1:1)
- (4-((6-(allyl(methyl)amino)hexyl)oxy)-2-fluorophenyl)(4-bromophenyl)methanone fumarate Ro48-8071
- Ro 48-8071 fumarate salt