177469-96-4
177469-96-4 structure
- Name: Implitapide
- Chemical Name: Implitapide
- CAS Number: 177469-96-4
- Molecular Formula: C35H37N3O2
- Molecular Weight: 531.687
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-02-25 10:40:43
- Modify Date: 2024-01-10 21:42:34
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Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.
| Name | Implitapide |
|---|---|
| Synonyms |
(2S)-2-Cyclopentyl-2-{3-[(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl)methyl]phenyl}-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
Q70OH404HR Benzeneacetamide, α-cyclopentyl-3-[(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl)methyl]-N-[(1R)-2-hydroxy-1-phenylethyl]-, (αS)- |
| Description | Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor. |
|---|---|
| Related Catalog | |
| Target |
MTP[1] |
| In Vitro | Implitapide suppresses MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC50=10 nM) and inhibit secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) with an IC50 value of 1.1 nM[1]. |
| In Vivo | 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[1]. |
| Animal Admin | Mice[1] Male apoE KO mice aged 6 weeks are fed either the CD or the WD. At age 7 weeks, apoE KO mice fed the WD are divided into two groups with similar mean body weight: apoE KO mice fed the WD and apoE KO mice fed the WD containing Implitapide (WI). Age-matched C57BL/6J mice fed the CD are used as a naive control (C57BL). Implitapide concentrations (14-22 ppm) in the diet are adjusted once a week to ensure dosage consumption of approximately 3.2 mg/kg/d. Body weight and average food consumption for 3 d are monitored weekly. Before and at 4 and 8 weeks of treatment, blood is collected for measurements of plasma lipid levels. At the 4th week, an oral fat-loading test is performed. At the 5th week of treatment, feces are collected for determination of fecal fat. At the end of 8 weeks of treatment, mice are euthanized for analysis of atherosclerotic lesions[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 739.3±60.0 °C at 760 mmHg |
| Molecular Formula | C35H37N3O2 |
| Molecular Weight | 531.687 |
| Flash Point | 400.9±32.9 °C |
| Exact Mass | 531.288574 |
| LogP | 6.70 |
| Vapour Pressure | 0.0±2.6 mmHg at 25°C |
| Index of Refraction | 1.653 |
| Storage condition | 2-8℃ |