IMPLITAPIDE
- CAS号:177469-96-4
- 英文名:Unii-Q70OH404hr
- 中文名:IMPLITAPIDE
- CBNumber:CB12493036
- 分子式:C35H37N3O2
- 分子量:531.69
- MOL File:177469-96-4.mol
- 沸点 :742.9±60.0 °C(Predicted)
- 密度 :1.21±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Solid
- 酸度系数(pKa) :14.22±0.10(Predicted)
- 颜色 :White to off-white
IMPLITAPIDE性质、用途与生产工艺
- 生物活性 Implitapide (AEGR 427) 是一种微粒体甘油三酯转移蛋白 (MTP) 抑制剂。
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靶点
MTP
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体外研究
Implitapide suppresses MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC 50 =10 nM) and inhibit secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) with an IC 50 value of 1.1 nM.
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体内研究
Implitapide (3.2 mg/kg/d) significantly reduces the plasma lipid levels to nearly or below the chow diet (CD) level at 4 and 8 weeks of treatment (p<0.01). Implitapide (3.2 mg/kg/d) markedly suppresses lipid-stained lesions in the mice fed the western-type diet (WD). Implitapide (3.2 mg/kg/d) significantly decreases lesion area by 83% compared with that of the WD group (p<0.01). ApoE KO mice fed a WD containing Implitapide (1, 5, and 15 mg/kg/d) for 14 weeks have been shown to reduce significantly both plaque area (by 66, 78, and 93%, respectively) and lipid moieties within plaque (4.3, 2.6, and 0%, respectively, versus 9.5% in controls). Implitapide at a dosage of approximately 3.2 mg/kg/d significantly reduces the lipid-stained aortic lesions by 83% in apoE KO mice.
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