网站主页 >> CAS数据库列表 >> 7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
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- CAS号:
- 189198-30-9
- 英文名:
- 2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo l-5-yl]acetic acid
- 英文别名:
- PactiMib;pactimibe;Pactimibe free base;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;1H-Indole-5-acetic acid, 7-[(2,2-dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-
- 中文名:
- 7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
- 中文别名:
- 帕替麦布;化合物 T28290;7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
- CBNumber:
- CB61261101
- 分子式:
- C25H40N2O3
- 分子量:
- 416.6
- MOL File:
- 189198-30-9.mol
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7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸化学性质
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沸点:
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604.4±55.0 °C(Predicted)
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密度:
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1.071
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储存条件:
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4°C, away from moisture
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溶解度:
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DMSO: 200 mg/mL (480.08 mM)
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酸度系数(pKa):
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4.00±0.10(Predicted)
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7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸性质、用途与生产工艺
Pactimibe sulfate (CS-505) 是一种 ACAT1/2 双重抑制剂,对于 ACAT1 的 IC50 值为 4.9 μM,对于 ACAT2 的 IC50 值为 3.0 μM。Pactimibe sulfate (CS-505) 抑制 ACAT,其 IC50 值在肝细胞中是 2.0 μM,在巨噬细胞中是 2.7 μM,在 THP-1 细胞中是 4.7 μM。Pactimibe sulfate (CS-505) 非竞争性抑制 oleoyl-CoA,Ki 是5.6 μM。此外,Pactimibe sulfate (CS-505) 明显抑制胆固醇酯的形成,IC50 是6.7 μM。Pactimibe sulfate (CS-505) 具有抗动脉粥样硬化的潜力,可降低血浆胆固醇的活性。
ACAT1
4.9 μM (IC
50
)
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ACAT2
3.0 μM (IC
50
)
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ACAT
2 μM (IC
50
, in the liver)
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ACAT
2.7 μM (IC
50
, in macrophages)
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ACAT
4.7 μM (IC
50
, in THP-1 cells)
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oleoyl-CoA
5.6 μM (Ki)
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cholesteryl ester formation
6.7 μM (IC
50
)
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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:
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Male C57BL/6J ApoE
−/−
mice aged 8-week-old
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Dosage:
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60 and 200 mg/kg/day
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Administration:
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Oral gavage; twice a day; 12 weeks
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Result:
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Decreased plasma cholesterol levels by 39% and 74% at the administration of 60 and 200 mg/kg/day.
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7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-100401 | Pactimibe | | 1 mg | 2045元 |
2024/04/30 | HY-100401 | 7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸 Pactimibe | 189198-30-9 | 5mg | 4500元 |
7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
生产厂家
189198-30-9, 7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸 相关搜索:
- C25H40N2O3
- 化合物 T28290
- 帕替麦布
- 7-[(2,2-二甲基-1-氧代丙基)氨基]-2,3-二氢-4,6-二甲基-1-辛基-1H-吲哚-5-乙酸
- 189198-30-9
- 1H-Indole-5-acetic acid, 7-[(2,2-dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-
- Pactimibe free base
- 7-[(2,2-Dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-1H-indole-5-acetic acid
- pactimibe
- PactiMib
- 2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo l-5-yl]acetic acid