CP-346086

CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC 50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo In Vitro CP-346086 (0.1-1000 nM) dose-dependently inhibits human MTP-mediated triglyceride transfer between vesicles with an IC 50 of 2.0 nM. CP-346086 (24 h) inhibits apolipoprotein B (apoB) and triglyceride secretion (IC 50 =2.6 nM) from Hep-G2 cells without affecting apoA-I secretion or lipid synthesis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CP-346086 (1-100 mg/kg; oral gavage once daily for 2 weeks) reduces plasma total, VLDL, and LDL cholesterol and triglycerides in mice . CP-346086 (25 mg/kg; a single p.o.) results in an almost complete inhibition of Tyloxapol-induced triglyceride accumulation in fasted rats . CP-346086 (0.1-10 mg/kg; a single p.o.) reduces acute plasma triglyceride in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: B6CBAF1J mice Dosage: 1, 2, 10, 20, 100 mg/kg Administration: Oral gavage once daily for 2 weeks Result: Lowered total, VLDL, and LDL cholesterol and triglycerides dose dependently with 23%, 33%, 75%, and 62% reductions at 10 mg/kg/day. Form:Solid IC50& Target:IC50: 2.0 nM (MTP)

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