LAB687

LAB687 (Compound 2a) is a Microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.9 nM for the secretion of apoB from HepG2 cells. LAB687 is also a Smoothened (Smo) antagonist with IC50s of 2.48 and 3.42 μM for mouse and human Smo receptor, respectively. LAB687 can lower the level of triglycerides and LDL cholesterol and inhibits the Hedgehog signaling pathway[1].

Product Specifications

CAS Number

[256397-11-2]

UNSPSC

12352005

Target

Hedgehog; Microsomal Triglyceride Transfer Protein (MTP) ; Smo

Related Pathways

Metabolic Enzyme/Protease; Stem Cell/Wnt

Field of Research

Cancer; Cardiovascular Disease

Smiles

COC(N[C@@H]1CC2=CC=C(C=C2C1)NC(C(C=CC=C3C)=C3C4=CC=C(C(F)(F)F)C=C4)=O)=O

Molecular Formula

C26H23F3N2O3

Molecular Weight

468.47

References & Citations

[1]Peukert S, et al. Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorg Med Chem Lett. 2009 Jan 15;19 (2) :328-31. |[2]Prashad M, et al. Process research and development of a MTP inhibitor: Another case of disappearing polymorphs upon scale-up[J]. Organic Process Research & Development, 2010, 14 (4) : 878-882.