产品
编 号：F602492
分子式：C25H40N2O3.1/2H2O4S
分子量：465.65
分子式：C25H40N2O3.1/2H2O4S
分子量：465.65
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 608510-47-0
产品详情
生物活性：
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s 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 Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
体内研究：
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.Animal Model:Male C57BL/6J ApoE?/? mice aged 8-week-old
Dosage: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.
体外研究：
Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation.
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s 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 Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
体内研究：
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.Animal Model:Male C57BL/6J ApoE?/? mice aged 8-week-old
Dosage: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.
体外研究：
Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation.
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