F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC 50 of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR , feedback-activates hepatic FXR , promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol , triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia.
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