| Description | Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A: cholesterol acyltransferase (ACAT), which can be used to study diseases due to high lipids. |
| In vitro | Lecimibide (DuP 128) (10 μM; 24 h) can inhibit 85% of the cellular esterification reaction in HepG2 cells.[1] |
| In vivo | Lecimibide (DuP 128) (2.2 mg/kg/day.; i.v) significantly reduced total plasma triglyceride and very low-density lipoprotein (VLDL) triglyceride concentrations in pigs fed high fat and cholesterol, respectively 36% and 31%. There were no significant effects on total cholesterol, VLDL cholesterol, LDL cholesterol, HDL cholesterol, or LDL apo B concentrations.[2] |
| Synonyms | DuP128, DuP-128, DuP 128 |
| molecular weight | 590.77 |
| Molecular formula | C34H40F2N4OS |
| CAS | 130804-35-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (93.1 mM) |
| References | 1. Wilcox LJ, et al. Secretion of hepatocyte apoB is inhibited by the flavonoids, naringenin and hesperetin, via reduced activity and expression of ACAT2 and MTP. J Lipid Res. 2001;42(5):725-734. 2. Burnett JR, et al. Inhibition of cholesterol esterification by DuP 128 decreases hepatic apolipoprotein B secretion in vivo: effect of dietary fat and cholesterol. Biochim Biophys Acta. 1998;1393(1):63-79. 3. Hainer JW, Terry JG, Connell JM, Zyruk H, Jenkins RM, Shand DL, Gillies PJ, Livak KJ, Hunt TL, Crouse JR 3rd. Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans. Clin Pharmacol Ther. 1994 Jul;56(1):65-74. PubMed PMID: 8033496. 4. Miyazaki A, Horiuchi S. [ACAT inhibitors]. Nihon Rinsho. 2001 Mar;59 Suppl 3:675-80. Review. Japanese. PubMed PMID: 11347152. |