Lomitapide

SKU: orb1300921

Description

Lomitapide is a potent small molecule inhibitor of microsomal triglyceride transfer protein (MTP), which is essential for assembling apoB-containing lipoproteins. It is widely used in research to investigate lipid metabolism, including in vitro cellular studies and in vivo models of dyslipidemia and fatty liver disease.

Research Area

Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 182431-12-5
• MW: 693.72
• Purity: 98.91%
• Formula: C₃₉H₃₇F₆N₃O₂
• SMILES: FC(F)(F)CNC(=O)C1(CCCCN2CCC(CC2)NC(=O)c2ccccc2-c2ccc(cc2)C(F)(F)F)c2ccccc2-c2ccccc12
• Target: Others,MTP,MTP
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:242 mg/mL (348.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.21 mM);Ethanol:93 mg/mL (134.06 mM)

Bioactivity

• Target IC50:
  MTP:8 nM
• In Vivo:
  Lomitapide, either as monotherapy or in combination with other lipid-lowering agents, notably reduces low-density lipoprotein cholesterol (LDL-C) levels by over 50%. However, its use is accompanied by significant gastrointestinal side effects and increased hepatic fat. The 50-mg capsule of lomitapide has a bioavailability of 7.1%, and its mean half-life is approximately 39.7 hours. Administration of a single dose of lomitapide can decrease serum triglycerides by 35% and 47% at dosages of 0.3 and 1 mg/kg, respectively. Moreover, multiple-dose regimens have shown a dose-dependent reduction in triglycerides (71%-87%), nonesterified fatty acids (33%-40%), and LDL-C (26-29%).
• In Vitro:
  Lomitapide is an oral microsomal triglyceride transfer protein (MTP) inhibitor indicated for the treatment of patients with HoFH, a rare form of hypercholesterolemia that can lead to premature atherosclerotic disease. Lomitapide undergoes hepatic metabolism through cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AEGR 733, AEGR733, AEGR-733, BMS 201038, BMS201038, BMS-201038, MTP, inhibit, Lomitapide, Inhibitor

Compound Identifiers

PubChem CID

9853053