E28362 is a selective PCSK9 antagonist that functions as an orally active lipid-lowering agent. By inhibiting the interaction between PCSK9 and the LDL receptor (LDLR), E28362 promotes the degradation of PCSK9 through the ubiquitin-proteasome pathway, leading to increased cell surface and total levels of LDLR. This mechanism enhances low-density lipoprotein uptake, resulting in significant reductions in plasma lipids, hepatic cholesterol, and triglyceride levels. E28362 also demonstrates minimal cytotoxicity at high concentrations and has been shown to substantially reduce atherosclerotic lesions in animal models, making it a valuable tool in studies of hyperlipidemia and atherosclerosis.
E28362 is a selective PCSK9 antagonist that functions as an orally active lipid-lowering agent. By inhibiting the interaction between PCSK9 and the LDL receptor (LDLR), E28362 promotes the degradation of PCSK9 through the ubiquitin-proteasome pathway, leading to increased cell surface and total levels of LDLR. This mechanism enhances low-density lipoprotein uptake, resulting in significant reductions in plasma lipids, hepatic cholesterol, and triglyceride levels. E28362 also demonstrates minimal cytotoxicity at high concentrations and has been shown to substantially reduce atherosclerotic lesions in animal models, making it a valuable tool in studies of hyperlipidemia and atherosclerosis.
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