Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ro 48-8071 fumarate is an inhibitor of OSC(Oxidosqualene cyclase; IC50=6.5 nM) that has low-density lipoprotein (LDL) cholesterol lowering activity.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 10,500 | |||
10 mg | 在庫あり | ¥ 16,000 | |||
25 mg | 在庫あり | ¥ 23,000 | |||
50 mg | 在庫あり | ¥ 29,000 | |||
100 mg | 在庫あり | ¥ 47,500 | |||
200 mg | 在庫あり | ¥ 62,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 12,500 |
説明 | Ro 48-8071 fumarate is an inhibitor of OSC(Oxidosqualene cyclase; IC50=6.5 nM) that has low-density lipoprotein (LDL) cholesterol lowering activity. |
ターゲット&IC50 | OSC:6.5 nM |
In vitro | Ro 48-8071 reduces cholesterol synthesis dose-dependently with an IC50 value of appr 1.5 nM in HepG2 cells[1]. 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[2]. 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[3]. |
In vivo | Ro 48-8071 effectively reduces LDL-C by approximately 60% at a dose of 150 μmol/kg per day without further decrease at up to 300 μmol/kg per day, while not affecting HDL-C levels at any dose in hamsters. At doses of 300 μmol/kg per day or higher, it significantly elevates MOS levels in the liver and markedly diminishes VLDL secretion in hamsters. Additionally, Ro 48-8071, at 5 or 20 mg/kg, substantially curtails in vivo tumor growth in mice and completely eliminates two out of 12 monitored tumors at 20 mg/kg, without causing weight loss in the mice. Furthermore, at 20 mg/kg/day, it achieves a rapid and enduring suppression of more than 50% in cholesterol synthesis in the entire small intestine of BALB/c mice, along with reductions in sterol synthesis in the large intestine and stomach. |
分子量 | 564.44 |
分子式 | C27H31BrFNO6 |
CAS No. | 189197-69-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (39.86 mM)
You can also refer to dose conversion for different animals. 詳細
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Ro 48-8071 fumarate 189197-69-1 Others Ro 48-8071 Fumarate Ro 488071 fumarate Ro 48 8071 fumarate Ro 48-8071 Inhibitor inhibit inhibitor