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

Properties

• 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
• 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: 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)
• InChI key: PTQXTEKSNBVPQJ-UHFFFAOYSA-N

Description

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).

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable