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CP-346086

Catalog No. T39303 CAS 186390-48-7

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.

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CP-346086, CAS 186390-48-7

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	MTP:2.0 nM (IC50)
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[1]. 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[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: B6CBAF1J mice[1]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.

Molecular Weight	477.491
Formula	C26H22F3N5O
CAS No.	186390-48-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CP-346086 186390-48-7 CP346086 CP 346086 inhibitor inhibit

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