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.
性状
Solid
IC50 & Target[1][2]
IC50: 2.0 nM (MTP)
体外研究(In Vitro)
CP-346086 (0.1-1000 nM) dose-dependently inhibits human MTP-mediated triglyceride transfer between vesicles with an IC50 of 2.0 nM.CP-346086 (24 h) inhibits apolipoprotein B (apoB) and triglyceride secretion (IC50=2.6 nM) from Hep-G2 cells without affecting apoA-I secretion or lipid synthesis. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Chandler CE, et, al. CP-346086: an MTP inhibitor that lowers plasma cholesterol and triglycerides in experimental animals and in humans. J Lipid Res. 2003 Oct;44(10):1887-901.