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目录号 : GC13231

An HNF4α antagonist

BI 6015 Chemical Structure

Cas No.:93987-29-2

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5mg
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10mg
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50mg
¥4,050.00
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Sample solution is provided at 25 µL, 10mM.

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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.

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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
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