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177469-96-4

177469-96-4 structure
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
  • 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

[1]. Ueshima K, et al. Implitapide, a microsomal triglyceride transfer protein inhibitor, reduces progression of atherosclerosis in apolipoprotein E knockout mice fed a Western-type diet: involvement of the inhibition of postprandial triglyceride elevation. Biol Pharm Bull. 2005 Feb;28(2):247-52.

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℃