CP-346086_product_DataBase

Bioactivity

CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo[1].

Target

IC50: 2.0 nM (MTP)

Invitro

CP-346086 (0.1-1000 nM) dose-dependently inhibits human MTP-mediated triglyceride transfer between vesicles with an IC50 of 2.0 nM[1].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[1].

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[1].CP-346086 (25 mg/kg; a single p.o.) results in an almost complete inhibition of Tyloxapol-induced triglyceride accumulation in fasted rats[1].CP-346086 (0.1-10 mg/kg; a single p.o.) reduces acute plasma triglyceride in mice[1]. Animal Model:

Name

CP-346086

CAS

186390-48-7

Formula

C26H22F3N5O

Molar Mass

477.48

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

CP-346086

CAS: 186390-48-7 F: C26H22F3N5O W: 477.48