生物活性 | |||
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描述 | Cell-based cotransfection assays have demonstrated that SR9238 is a synthetic inverse agonist for LXR, with IC50 values of 214 nM for LXRα and 43 nM for LXRβ. SR9238 also effectively inhibits the transcription of a luciferase reporter gene driven by the Fasn promoter. It has been found that SR9238 induces an increase in the interaction of CoRNR box peptides derived from NCoR (NCoR ID1 and NCoR ID2) with LXRα and LXRβ, while decreasing the interaction with coactivator NR box peptides derived from TRAP220. The recruitment of CoRNR box peptides induced by SR9238 is dose-dependent for both LXRα and LXRβ. Treatment of HepG2 cells with SR9238 results in a significant reduction in the expression of Fasn and Srebp1c mRNA[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.68mL 0.34mL 0.17mL |
8.39mL 1.68mL 0.84mL |
16.79mL 3.36mL 1.68mL |
参考文献 |
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