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D4-abiraterone

产品编号 T10946Cas号 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.

D4-abiraterone

D4-abiraterone

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

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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2 mg¥ 1,4805日内发货
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产品介绍

生物活性
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
化学信息
分子量347.49
分子式C24H29NO
CAS No.154229-21-7
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (143.89 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.8778 mL14.3889 mL28.7778 mL143.8890 mL
5 mM0.5756 mL2.8778 mL5.7556 mL28.7778 mL
10 mM0.2878 mL1.4389 mL2.8778 mL14.3889 mL
20 mM0.1439 mL0.7194 mL1.4389 mL7.1945 mL
50 mM0.0576 mL0.2878 mL0.5756 mL2.8778 mL
100 mM0.0288 mL0.1439 mL0.2878 mL1.4389 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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
%
%Tween 80
%ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

关键词

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