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Merck

PZ0190

Avasimibe

≥98% (HPLC)

Synonym(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

Empirical Formula (Hill Notation):
C29H43NO4S
CAS Number:
166518-60-1
Molecular Weight:
501.72
UNSPSC Code:
12352200
PubChem Substance ID:
329823764
MDL number:
MFCD00934956
NACRES:
NA.28

Product Name

Avasimibe, ≥98% (HPLC)

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)

SMILES string

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 key

PTQXTEKSNBVPQJ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to tan

solubility

DMSO: ≥40 mg/mL

relevant disease(s)

Alzheimer′s disease; cardiovascular diseases

storage temp.

room temp

Quality Level

100

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.

Biochem/physiol Actions

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000508970
0000508970
0000351974
0000351974
0000237848

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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
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.
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
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
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
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