Lomitapide, Microsomal triglyceride transfer protein inhibitor

Product Details

Formal Name: N-(2,2,2-Trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide

Alternate Names: AEGR-733; BMS-201038

Molecular Formula: C₃₉H₃₇F₆N₃O₂

Formula Weight: 693.7

CAS Number: 182431-12-5

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to 50 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Microsomal triglyceride transfer protein inhibitor

Functions

Potent (IC₅₀ = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia. It has displayed anticancer activity acting through various pathways including autophagy-dependent cancer cell death via direct inhibition of the kinase activity of mTORC1, activation of AMPK/Beclin1-mediated autophagy, Notch inhibition via targeting TACE and γ-secretase, blocking ZDHHC5-dependent palmitoylation on SSTR5, PFKFB3 inhibition, and PARP14/DRP1-mediated mitophagy.

Application Procedures

First dissolved in DMSO (50 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)