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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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Colin Berry et al.
Circulation, 115(14), 1851-1857 (2007-03-29)
The relative merits of quantitative coronary analysis (QCA) and intravascular ultrasound (IVUS) for the assessment of progression/regression in coronary artery disease are uncertain. To explore this subject further, we analyzed the angiographic and IVUS data derived from a contemporary clinical
Akira Miyazaki et al.
Current drug targets. Cardiovascular & haematological disorders, 5(6), 463-469 (2006-03-01)
Acyl-coenzyme A: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes the formation of cholesterol esters from cholesterol and fatty acyl-coenzyme A. Animal experiments showed that ACAT inhibitors reduce plasma cholesterol levels by suppressing absorption of dietary cholesterol and by
Jasminder Sahi et al.
The Journal of pharmacology and experimental therapeutics, 306(3), 1027-1034 (2003-05-27)
In vitro and clinical studies were conducted to characterize the potential of avasimibe, an acyl-CoA/cholesterol acyltransferase inhibitor to cause drug-drug interactions. Clinically, 3- and 6-fold increases in midazolam (CYP3A4 substrate) oral clearance were observed after 50 and 750 mg of
Marcelo F Di Carli et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 52(9), 1369-1377 (2011-08-19)
The metabolic syndrome affects 25% of the U.S. population and greatly increases the risk of diabetes and coronary artery disease (CAD). We tested the hypothesis that the metabolic syndrome is associated with impaired coronary vasodilator function, a marker of atherosclerotic
Stephen G Worthley et al.
Pathophysiology of haemostasis and thrombosis, 36(1), 9-17 (2008-03-12)
The ability to modify the enzymatic processes involved in promoting atherosclerotic plaque disruption and to serially monitor atherosclerotic evolution could provide novel information in the management of patients with atherosclerosis. We studied the effects of a statin (atorvastatin) and its
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