Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Abiraterone (CB-7598) 是不可逆的CYP17A1抑制剂,具有抗雄激素作用,抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶 (IC50:2.5 nM) 和 17,20-裂合酶 (IC50:15 nM) 活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 398 | 现货 | ||
50 mg | ¥ 1,169 | 现货 | ||
100 mg | ¥ 1,775 | 现货 | ||
200 mg | ¥ 2,366 | 现货 | ||
500 mg | ¥ 3,990 | 现货 | ||
1 g | ¥ 5,790 | 现货 |
产品描述 | Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM). |
靶点活性 | CYP17:2 nM |
体外活性 | Abiraterone对睾丸激素水平的降低效果几乎切除睾丸的效果相同.Abiraterone对任何器官尺寸均无明显降低作用.Abiraterone可抑制人类睾丸微粒体中CYP17(IC50:72 nM).与对照组相比,Abiraterone 降低 95%以上睾丸激素水平. |
体内活性 | Abiraterone抑制体外增殖和雄激素受体调节的雄激素受体阳性前列腺癌细胞基因表达,这可能是通过抑制类固醇和抗雄激素受体实现的。更高浓度的Abiraterone抑制依普利酮激活的突变型雄激素受体。Abiraterone 取代WT-AR(EC50:13.4 μM)和T877A(EC50:7.9 μM)中的配体。Abiraterone醋酸盐明显抑制T分泌(48%),且可使LH浓度达到192%。Abiraterone抑制大鼠睾丸微粒的裂解酶活性(IC50:5.8 nM)。 |
激酶实验 | C17,20-lyase activity assay: Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contained 0.25 M sucrose, 20 mM Tris–HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, Abiraterone is evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at ?20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format using a specific antibody against Δ4A. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a 1450 MicrobetaPlus liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration. |
细胞实验 | LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence.(Only for Reference) |
别名 | 阿比特龙, CB-7598 |
化合物与蛋白结合的复合物 |
Zebra fish cytochrome P450 17A2 with Abiraterone |
分子量 | 349.51 |
分子式 | C24H31NO |
CAS No. | 154229-19-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 5.4 mg/mL (15.45 mM), sonification is recommended.
DMF: 8.75 mg/mL (25.04 mM), sonification/heating is recommended.
DMSO: 5 mg/mL (14.31 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMF / DMSO | 1 mM | 2.8611 mL | 14.3057 mL | 28.6115 mL | 71.5287 mL |
5 mM | 0.5722 mL | 2.8611 mL | 5.7223 mL | 14.3057 mL | |
10 mM | 0.2861 mL | 1.4306 mL | 2.8611 mL | 7.1529 mL | |
DMF | 20 mM | 0.1431 mL | 0.7153 mL | 1.4306 mL | 3.5764 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。
Abiraterone 154229-19-3 Metabolism P450 Inhibitor Cytochrome P450 CB 7598 inhibit CYPs 阿比特龙 CB7598 CB-7598 inhibitor