Pactimibe sulfate

Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC 50 s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) 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 sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a K i value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC 50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity . In Vitro Pactimibe sulfate (CS-505) 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 sulfate (CS-505; 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. 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|)

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet