MTP (Microsomal Triglyceride Transfer Protein,微粒体甘油三酯转移蛋白)是一种内质网膜蛋白,主要负责脂质的转运和脂蛋白的组装。MTP在肝脏、肠道和脂肪细胞中表达,通过将甘油三酯和胆固醇酯转移到新生的脂蛋白颗粒中,促进脂蛋白的成熟和分泌。MTP能够调节血液中的甘油三酯和胆固醇水平,其功能异常与多种脂质代谢紊乱相关,如家族性低β脂蛋白血症和心血管疾病。
CP-346086 is a highly potent and orally bioavailable inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM against both human and rodent MTP. This compound effectively reduces plasma levels of cholesterol and triglycerides when administered in vivo.
CP-346086 dihydrate is a potent and orally active inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM for both human and rodent MTP. This compound effectively lowers plasma cholesterol and triglyceride levels in vivo.