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Implitapide (Synonyms: AEGR 427)

Cat. No.: HY-106130
Handling Instructions

Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.

For research use only. We do not sell to patients.

Implitapide Chemical Structure

Implitapide Chemical Structure

CAS No. : 177469-96-4

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Description

Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.

IC50 & 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].

Clinical Trial
Molecular Weight

531.69

Formula

C₃₅H₃₇N₃O₂

CAS No.

177469-96-4

SMILES

CC1=C(C2=C3C=CC=C2)C(N3CC4=CC=C([[email protected]](C5CCCC5)C(N[[email protected]](C6=CC=CC=C6)CO)=O)C=C4)=NC(C)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Implitapide
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