189198-30-9
189198-30-9 結(jié)構(gòu)式
基本信息
7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氫-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
pactimibe
2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo l-5-yl]acetic acid
7-[(2,2-Dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-1H-indole-5-acetic acid
物理化學(xué)性質(zhì)
常見問題列表
|
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 ) |
Pactimibe sulfate (CS-505) induces moderate ACAT inhibition in monocyte-derived macrophages, leading to the suppression of foam cell formation.
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. |