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Avasimibe

Chemical Structure : Avasimibe

CAS No.: 166518-60-1

Avasimibe (CI-1011;PD-148515;CI1011;PD148515;CI 1011;PD 148515)

Catalog No.: PC-43398Not For Human Use, Lab Use Only.

Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Avasimibe (CI-1011, PD-148515) is a potent, selective inhibitor of acyl-CoA: cholesterol O-acyl transferase (ACAT) with IC50 of 60 nM; potently reduces plasma cholesterol in chow-fed rats and in rabbits fed a cholesterol-free, casein-containing diet characterized by both hepatic overproduction of apo B-containing lipoproteins and delayed lipoprotein clearance; decreases both VLDL and LDL apolipoprotein B production in miniature pigs; synergistically reduces cholesteryl ester content in THP-1 macrophages combined with Atorvastatin,

Dyslipidemia

Phase 3 Discontinued

Physicochemical Properties

M.Wt 501.72102
Formula C29H43NO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 28 mg/mL

Chemical Name/SMILES

Sulfamic acid, N-[2-[2,4,6-tris(1-methylethyl)phenyl]acetyl]-, 2,6-bis(1-methylethyl)phenyl ester

References

1. Lee HT, et al. J Med Chem. 1996 Dec 20;39(26):5031-4.

2. Ramharack R, et al. Atherosclerosis. 1998 Jan;136(1):79-87.

3. Burnett JR, et al. J Lipid Res. 1999 Jul;40(7):1317-27.

4. Llaverías G, et al. Eur J Pharmacol. 2002 Sep 6;451(1):11-7.

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