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PZ0190

Sigma-Aldrich

Avasimibe

≥98% (HPLC)

Synonyme(s) :

CI-1011; PD 148515; [[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl)phenyl ester] sulfamic acid

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About This Item

Formule empirique (notation de Hill):
C29H43NO4S
Numéro CAS:
166518-60-1
Poids moléculaire :
501.72
Numéro MDL:
MFCD00934956
Code UNSPSC :
12352200
ID de substance PubChem :
329823764

Niveau de qualité

100

Essai

≥98% (HPLC)

Forme

powder

Couleur

white to tan

Solubilité

DMSO: ≥40 mg/mL

Maladie(s) pertinente(s)

Alzheimer′s disease; cardiovascular diseases

Température de stockage

room temp

Chaîne SMILES 

CC(C)c1cc(C(C)C)c(CC(=O)NS(=O)(=O)Oc2c(cccc2C(C)C)C(C)C)c(c1)C(C)C

InChI

1S/C29H43NO4S/c1-17(2)22-14-25(20(7)8)27(26(15-22)21(9)10)16-28(31)30-35(32,33)34-29-23(18(3)4)12-11-13-24(29)19(5)6/h11-15,17-21H,16H2,1-10H3,(H,30,31)

Clé InChI

PTQXTEKSNBVPQJ-UHFFFAOYSA-N

Catégories apparentées

Application

Avasimibe has been used as an inhibitor of acyl-coenzyme A: cholesterol acyltransferase (ACAT) in Huh7.5.1 cells for testing its combination with direct-acting antivirals (DAAs) and to test its effect on lipid droplet accumulation in acidosis-adapted cancer cells. It may be used as an inhibitor of ACAT to assess cholesterol esterification in Trypanosoma cruzi.

Actions biochimiques/physiologiques

Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor. It was originally developed as an antilepic drug, and was shown to significantly reduce plasma total triglyceride and VLDL-cholesterol, but later clinical trials were disappointing. ACAT has also been investigated as a potential therapeutic target for Alzheimer′s disease. Recent studies have looked at the effects of avasimibe in reducing amyloid pathology by limiting generation and increasing clearance of diffusible amyloid-beta (Abeta).
Avasimibe is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor

Informations légales

Sold for research purposes under agreement from Pfizer Inc.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000351974
0000351974
0000237848
0000237848
0000184190

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Consulter la Bibliothèque de documents

Jasminder Sahi et al.
Drug metabolism and disposition: the biological fate of chemicals, 32(12), 1370-1376 (2004-08-31)
Avasimibe, an acyl-CoA:cholesterol acyltransferase inhibitor, has been previously shown to be a potent inducer of CYP3A4 and multiple drug resistance protein 1. We have further characterized the drug interaction potential of avasimibe by studying the inductive and inhibitory effect of
William R Hiatt et al.
Vascular medicine (London, England), 9(4), 271-277 (2005-02-01)
This study tested the hypothesis that avasimibe, an inhibitor of acyl coenzyme A-cholesterol acyltransferase (ACAT), would improve treadmill exercise performance in patients with claudication secondary to peripheral arterial disease (PAD). Four hundred and forty-two patients with PAD (ankle-brachial index in
Frederick J Raal et al.
Atherosclerosis, 171(2), 273-279 (2003-12-04)
This study assessed the efficacy and safety of avasimibe (CI-1011), an inhibitor of acyl coenzyme A-cholesterol acyltransferase (ACAT) in subjects with homozygous familial hypercholesterolemia (HoFH). Twenty seven subjects were enrolled in a double-blind, randomized, 3-sequence crossover trial of atorvastatin 80
Yves Rival et al.
DNA and cell biology, 23(5), 283-292 (2004-06-01)
It is now recognized that atherosclerosis complications are related to the unstable character of the plaque rather than its volume. Vulnerable plaques often contain a large lipid core, a reduced content of smooth muscle cells, and accumulation of inflammatory cells.
Jean-Claude Tardif et al.
Circulation, 110(21), 3372-3377 (2004-11-10)
Inhibition of the acyl coenzyme A:cholesterol acyltransferase (ACAT) enzyme may prevent excess accumulation of cholesteryl esters in macrophages. The ACAT inhibitor avasimibe was shown to reduce experimental atherosclerosis. This study was designed to investigate the effects of avasimibe on human
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