BI 6015
目录号 : GC13231An HNF4α antagonist
Cas No.:93987-29-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BI 6015 is an antagonist of hepatocyte nuclear factor 4α [1].
Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor and regulates gene expression in enterocytes, hepatocytes and pancreatic β cells [1].
BI 6015 is a HNF4α antagonist. BI6015 inhibited the insulin promoter. In T6PNE cells, BI6015 reduced the expression of endogenous insulin by 50-fold. In MIN6 and HepG2 cells, BI6015 inhibited the expression of HNF4α. Also, BI6015 changed HNF4α protease sensitivity [1]. In T6PNE cells, BI 6015 reduced the levels of longer chain acylcarnitines (C18, C18:1, C16, and C14) and increased acetylcarnitine, which suggested that BI 6015 increased fatty acid oxidation. In the human hepatoma cell line Hep3B, BI 6015 exhibited cytotoxic activity [1].
In mice, BI6015 (30 mg/kg) induced a loss of HNF4α protein in the liver, but not in the kidney and intestine. Also, BI6015 caused fat accumulation and steatosis and vesicular changes in a dose-dependent way [1].
Reference:
[1]. Kiselyuk A, Lee SH, Farber-Katz S, et al. HNF4a Antagonists Discovered by a High-Throughput Screen for Modulators of the Human Insulin Promoter. Chem Biol, 2012, 19(7): 806-818.
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.018 mL | 15.0898 mL | 30.1796 mL |
5 mM | 0.6036 mL | 3.018 mL | 6.0359 mL |
10 mM | 0.3018 mL | 1.509 mL | 3.018 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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