生物活性 | |||
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描述 | Triacylglycerol hydrolase (TGH) is a lipase involved in the mobilization of triglycerides for assembly into very-low-density lipoprotein. GR148672X is a TGH inhibitor with an IC50 value of 4nM. GR148672X at a concentration of 5μM did not affect the enzymatic activity of lipoprotein lipase. Oral administration of normal-fed hamsters with GR148672X (25mg/kg, twice a day) for 3 days led to a significant reduction in plasma concentrations of triglyceride (–55% versus the solvent-treated animals), VLDULDL cholesterol (–40 % versus the solvent-treated animals), and apolipoprotein B-100, while the levels of high-density lipoprotein cholesterol were not significantly affected.[2] | ||
作用机制 | GR148672X is a specific TGH inhibitor.[2] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.94mL 0.59mL 0.29mL |
14.69mL 2.94mL 1.47mL |
29.38mL 5.88mL 2.94mL |
参考文献 |
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[2]Method of screening for triacyglycerol hydrolase inhibitors |