| Description | PD 128042 (CI 976) is a potent orally active and selective ACAT inhibitor(IC50: 73 nM) and a potent lysophospholipid acyltransferase(LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps. |
| In vitro | In the chronic cholesterol-fed rat model, CI 976 decreases non-high density lipoprotein (HDL)-cholesterol and increases HDL-cholesterol in rats with pre-established dyslipidemia[4]. |
| Target activity | Golgi-associated LPAT:15 μM, ACAT:73 nM |
| Synonyms | CI 976 |
| molecular weight | 393.56 |
| Molecular formula | C23H39NO4 |
| CAS | 114289-47-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/ml(63.52 mM) DMF: 25 mg/ml(63.52 mM) Ethanol: 25 mg/ml(63.52 mM) |
| References | 1. Chambers K, et al. A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways. J Cell Sci. 2005;118(Pt 14):3061-3071. 2. O'Brien PM, et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J Med Chem. 1994;37(12):1810-1822. 3. Drecktrah D, et al. Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol Biol Cell. 2003;14(8):3459-3469. 4. Krause BR, et al. In vivo evidence that the lipid-regulating activity of the ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT. J Lipid Res. 1993;34(2):279-294. |
| Citations | 1. Luo W, Chen L, Sun H, et al.Soat2 inhibitor avasimibe alleviates acute pancreatitis by suppressing acinar cell ferroptosis.Naunyn-Schmiedeberg's Archives of Pharmacology.2024: 1-11. |