生物活性 | |||
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描述 | RP-64477 is identified as a powerful inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT), an enzyme essential for cholesterol esterification. It demonstrates inhibitory effects across a variety of species and tissues, with IC50 values ranging from 6 to 283 nM, indicating a broad spectrum of activity without noticeable differences between species or tissues. Additionally, RP-64477 shows significant inhibition in human cell lines derived from hepatic (HepGZ), intestinal (CaCo-2), and monocytic (THP-1) origins, with IC50s of 503, 113, and 180 nM, respectively. It does not inhibit rat PCEH or LCAT up to concentrations of 200 μM and 20 μM, respectively[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.01mL 0.40mL 0.20mL |
10.03mL 2.01mL 1.00mL |
20.05mL 4.01mL 2.01mL |
参考文献 |
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