Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ro 48-8071 fumarate 是一种氧化鲨烯环化酶抑制剂(IC50:6.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 355 | 现货 | ||
10 mg | ¥ 652 | 现货 | ||
100 mg | ¥ 1,996 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 462 | 现货 |
产品描述 | Ro 48-8071 fumarate is an inhibitor of OSC(Oxidosqualene cyclase; IC50=6.5 nM) that has low-density lipoprotein (LDL) cholesterol lowering activity. |
靶点活性 | OSC:6.5 nM |
体外活性 | 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]. |
体内活性 | 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[1]. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Moreover, 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[2]. 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 in the large intestine and stomach is also reduced[4]. |
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)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7717 mL | 8.8583 mL | 17.7167 mL | 44.2917 mL |
5 mM | 0.3543 mL | 1.7717 mL | 3.5433 mL | 8.8583 mL | |
10 mM | 0.1772 mL | 0.8858 mL | 1.7717 mL | 4.4292 mL | |
20 mM | 0.0886 mL | 0.4429 mL | 0.8858 mL | 2.2146 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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