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D4-abiraterone

D4-abiraterone

产品编号 T10946   CAS 154229-21-7
别名: Abiraterone D4A metabolite, CB-7627, Δ4-Abiraterone

D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.

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D4-abiraterone Chemical Structure
D4-abiraterone, CAS 154229-21-7
规格 价格/CNY 货期 数量
2 mg ¥ 1,480 5日内发货
产品目录号及名称: D4-abiraterone (T10946)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.
体外活性 D4-Abiraterone (D4A) (10 mM) almost completely prevented the conversion of D4-androstenedione (AD) to 5α-androstanedione and other 5α-reducing androgens. D4-Abiraterone has greater affinity for androgen receptor (AR) than mutant (expressed in LNCaP, half maximum inhibitory concentration (IC50 = 5.3 nM)) and wild type (expressed in LAPC4, IC50 = 7.9 nM) Abiron (IC50 = 418 and> 500 nM, respectively). Compared with Abi, D4-abiraterone significantly inhibited the expression of PSA, TMPRSS2 and FKBP5 in LNCAP, LAPC4 and C4-2 cell lines. D4-Abiraterone also suppressed AR target gene expression in a dose-dependent manner.
体内活性 In preventing the conversion of 3β-hydroxysteroid dehydrogenase (3βHSD) from dehydroepiandrosterone (DHEA) to D4-androstenedione (AD) in LNCaP and VCaP xenografts, D4-Abiraterone (D4A) The effect is ten times higher than that of Abiron. In LNCaP and VCaP xenografts, AD accumulation was blocked at 48 h, and 0.1 μMD4-Abiraterone was equivalent to 1 μMAbi. Compared with the Abirate acetate group, the progress of the D4-Abiraterone group was significantly delayed (P = 0.011). Compared with abirate acetate, D4-Abiraterone treatment can increase progression-free survival .
别名 Abiraterone D4A metabolite, CB-7627, Δ4-Abiraterone
分子量 347.49
分子式 C24H29NO
CAS No. 154229-21-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (143.89 mM), sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8778 mL 14.3889 mL 28.7778 mL 71.9445 mL
5 mM 0.5756 mL 2.8778 mL 5.7556 mL 14.3889 mL
10 mM 0.2878 mL 1.4389 mL 2.8778 mL 7.1945 mL
20 mM 0.1439 mL 0.7194 mL 1.4389 mL 3.5972 mL
50 mM 0.0576 mL 0.2878 mL 0.5756 mL 1.4389 mL
100 mM 0.0288 mL 0.1439 mL 0.2878 mL 0.7194 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Li Z, et al. Conversion of abiraterone to D4A drives anti-tumour activity in prostate cancer. Nature. 2015 Jul 16;523(7560):347-51.
Dehydroisoandrosterone 3-acetate Darolutamide CSRM617 hydrochloride BMS-564929 GSK-2881078 Testosterone undecanoate Lupeol RU 59063

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

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。

Keywords

D4-abiraterone 154229-21-7 Endocrinology/Hormones Androgen Receptor Abiraterone D4A metabolite CB-7627 CB7627 CB 7627 D4abiraterone D-4-abiraterone Δ4-Abiraterone D4 abiraterone delta4-Abiraterone Inhibitor inhibitor inhibit

 

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