Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC 50 s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC 50 s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a K i value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC 50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity . In Vitro Pactimibe (CS-505 free base) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Pactimibe (CS-505 free base; 60 and 200 mg/kg/day; oral gavage; twice a day; 12 weeks) induces an inhibition for ACAT-1 and ACAT-2, causing a reduction of plasma cholesterol but no influence on macrophage- or collagen-positive areas. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J ApoE −/− mice aged 8-week-oldDosage: 60 and 200 mg/kg/day Administration: Oral gavage; twice a day; 12 weeks Result: Decreased plasma cholesterol levels by 39% and 74% at the administration of 60 and 200 mg/kg/day Form:Solid IC50& Target:ACAT1|4.9 μM (IC|50|)|ACAT2|3.0 μM (IC|50|)|ACAT|2 μM (IC|50|, in the liver)|ACAT|2.7 μM (IC|50|, in macrophages)|ACAT|4.7 μM (IC|50|, in THP-1 cells)|oleoyl-CoA|5.6 μM (Ki)|cholesteryl ester formation|6.7 μM (IC|50|)
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Pactimibe
CAS number：189198-30-9 molecular formula：C25H40N2O3
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| Chinese alias | 帕麦布 | ||
| English alias | MS-27258 | DTXSID80172315 | 2-[7-(2,2-Dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo L-5-yl]acetic acid | N-(1-Octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2-dimethylpropanamide | N-(1-Octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2 | ||
| CAS number | 189198-30-9 | molecular formula | C25H40N2O3 |
| molecular weight | 416.60 g/mol | Exact mass | ≥98% |
| PSA | 69.600 Ų | logp | 6.3 |
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