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Biochem/physiol Actions
ATP citrate-lyase inhibitor SB-201076 γ-lactone prodrug with cell-permeability, oral availability and in vivo hypocholesterolaemic/hypolipidaemic efficacy.
SB-204990 is a cell-permeable and orally available γ-lactone prodrug of the non-cell-permeable SB-201076 that inhibits human and rat ATP citrate-lyase (Ki =1 μM against human and rat ACL) in a predominantly competitive manner with a small but significant uncompetitive component. SB-204990 treatment is shown to suppress the rate of cellular cholesterol and fatty acid synthesis in HepG2 cultures (by 91% & 82%, respectively, with 30 μM SB-204990), and display hypocholesterolaemic and hypolipidaemic efficacy in vivo when administered in the diet (0.05-0.25%, w/w; mice, rats, dogs).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | Clc1c(ccc(c1)Cl)CCCCCC[C@H]2OC(=O)[C@@](C2)(O)CC(=O)O |
| InChI | 1S/C18H22Cl2O5/c19-13-8-7-12(15(20)9-13)5-3-1-2-4-6-14-10-18(24,11-16(21)22)17(23)25-14/h7-9,14,24H,1-6,10-11H2,(H,21,22)/t14-,18+/m1/s1 |
| InChI key | YTRNLFYTHYWDAU-KDOFPFPSSA-N |
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