CP-346086 dihydrate_product_DataBase

Bioactivity	CP-346086 dihydrate 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 dihydrate 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 dihydrate
CAS	1262769-98-1
Formula	C26H26F3N5O3
Molar Mass	513.51
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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