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CP 346086
- Soluble in DMSO
- MF: C26H22F3N5O
- MW: 477.48
Description
CP 346086 is a potent microsomal triglyceride transfer protein (MTP/MTTP) inhibitor with reported IC50 of 2.0 nM against both human and rodent MTP activity. It reduces total cholesterol, LDL cholesterol and triglycerides in treatment studies with little change in HDL cholesterol.
MTP is required for apoB-containing lipoprotein assembly and triglyceride transfer in liver and intestine. CP 346086 is relevant for lipid-lowering pharmacology and comparisons with other MTP inhibitors such as lomitapide and SLX 4090.
Key Features
- Potent MTP/MTTP inhibitor
- Nanomolar activity in human and rodent MTP assays
- Reduces LDL cholesterol and triglyceride levels in reported studies
- More potent than comparator MTP inhibitors in cited assays
Applications
- MTP enzyme assays
- Lipoprotein assembly research
- Lipid-lowering pharmacology studies
- Cholesterol and triglyceride metabolism models
More Information
| Parent CAS No. | 186390-48-7 |
|---|---|
| Chemical Name | N-(2-((1H-1,2,4-triazol-5-yl)methyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide |
| extra_info | . |
| SMILES | C12CCN(CC3NC=NN=3)CC=1C=CC(NC(=O)C1C=CC=CC=1C1C=CC(C(F)(F)F)=CC=1)=C2 |
| MFCD | N.A. |
| InChi | InChI=1S/C26H22F3N5O/c27-26(28,29)20-8-5-17(6-9-20)22-3-1-2-4-23(22)25(35)32-21-10-7-19-14-34(12-11-18(19)13-21)15-24-30-16-31-33-24/h1-10,13,16H,11-12,14-15H2,(H,32,35)(H,30,31,33) |
| InChiKey | WNDIAFXQKOHFLV-UHFFFAOYSA-N |
| CID | 9826309 |
| Short Description | MTP inhibitor |
References
- C.E. Chandler et al. CP-346086: an MTP inhibitor that lowers plasma cholesterol and triglycerides in experimental animals and in humans. J. Lipid. Res. 2003, 44, 1887-1901.
- E. Kim et al. A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J. Pharmacol. Exp. Ther. 2011, 337, 775-785.
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