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网站主页 化工产品目录 生物化工 抑制剂 代谢(Metabolism) P450 (e.g. CYP17) 抑制剂 阿比特龙 阿比特龙
  • 阿比特龙|T6216

阿比特龙|T6216

Abiraterone
154229-19-3
398 10mg 起订
1169 50mg 起订
1775 100mg 起订
上海 更新日期:2024-09-14

TargetMol中国(陶术生物)

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产品详情:

中文名称:
阿比特龙
英文名称:
Abiraterone
CAS号:
154229-19-3
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.87%
产品类别:
抑制剂
货号:
T6216

Product Introduction

Bioactivity

名称Abiraterone
描述Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).
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)
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.
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)。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 5.4 mg/mL (15.45 mM), Sonication is recommended.
DMF : 8.75 mg/mL (25.04 mM), Sonication and heating are recommended.
DMSO : 1 mg/mL, Sonication is recommended.
关键字Inhibitor | Cytochrome P450 | CB 7598 | inhibit | CYPs | CB7598 | Abiraterone
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相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | FDA 上市药物库 | 抗癌药物库
阿比特龙|||CB-7598|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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