|Related Categories||A to C, Acyl-CoA Cholesterol Acyltransferase, Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Biochemicals and Reagents,|
|solubility||DMSO: soluble16 mg/mL|
human ... SOAT1(6646)|
rat ... Soat1(81782)
Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor.
Sandoz 58-035 inhibits the accumulation of cholesteryl esters and inhibits the esterification of cholesterol by 95% in arterial smooth muscle cells in culture.1 It does not affect the triglyceride metabolism by the gut.2
Sandoz 58-035 was used to induce simultaneous activation of unfolded protein response (UPR) and pattern recognition receptors (PRRs) in mouse peritoneal macrophages.3
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≥97.0% (HPLC), powder
>98% (HPLC), solid
Download BioFiles v7 n5 (3.18 Mb PDF) Back to Pharmaceutical Drugs and Drug Candidates homepage
BioFiles v7 n5, 2012, 21–24
Keywords: Anti-inflammatory agents, Cardiovascular, Chemical vapor deposition, Clinical, Diabetes, Inflammation, Oxidations, Pharmaceutical, Transcription
To more efficiently transport both dietary and synthesized cholesterol, it is converted to cholesteryl esters. Free cholesterol can be taken up by lipoproteins, but is confined to the outer surface o...
BioFiles 2007, 2.7, 10.
Reduced cholesterol transmucosal transport in rats with inhibited mucosal acyl CoA:cholesterol acyltransferase and normal pancreatic function. Clark SB and Tercyak AM J. Lipid Res. 25(2), 148-59, (1984)
Free cholesterol overloading induced smooth muscle cells death and activated both ER- and mitochondrial-dependent death pathway. Kedi X, Ming Y, Yongping W, et al. Atherosclerosis 207(1), 123-30, (2009)
Decreased intracellular degradation and increased secretion of apo B-100 in Hep G2 cells after inhibition of cholesteryl ester synthesis. Ooyen C, Zecca A, Zanelli T, et al. Atherosclerosis 130(1-2), 143-52, (1997)
Application of 2-hydroxypropyl-beta-cyclodextrin in the assay of acyl-CoA:cholesterol acyltransferase and neutral and acid cholesterol ester hydrolases. Liza M, Romero JR, Chico Y, et al. Lipids 31(3), 323-9, (1996)
Evidence for a lack of regulation of the assembly and secretion of apolipoprotein B-containing lipoprotein from HepG2 cells by cholesteryl ester. Wu X, Sakata N, Lui E, et al. J. Biol. Chem. 269(16), 12375-82, (1994)
Cholesterol esterification plays a major role in determining low-density-lipoprotein receptor activity in primary monolayer cultures of rat hepatocytes. Salter AM, Ekins N, al-Seeni M, et al. Biochem. J. 263(1), 255-60, (1989)
Accumulation of oleate-rich cholesteryl esters by acetyl-LDL in macrophages in the presence of an acyl-CoA: cholesterol acyltransferase inhibitor (Sandoz 58-035). Shimasaki O, Mineo C, Mowri H, et al. Biochem. Int. 20(2), 389-96, (1990)
The prototypical inhibitor of cholesterol esterification, Sah 58-035 [3-[decyldimethylsilyl]-n-[2-(4-methylphenyl)-1-phenylethyl]propanamide], is an agonist of estrogen receptors. de Medina P, Boubekeur N, Balaguer P, et al. J. Pharmacol. Exp. Ther. 319(1), 139-49, (2006)
Neutral-lipid analysis reveals elevation of acylglycerols and lack of cholesterol esters in Plasmodium falciparum-infected erythrocytes. Nawabi P, Lykidis A, Ji D, et al. Eukaryotic Cell 2(5), 1128-31, (2003)
Novel effects of the acyl-coenzyme A:Cholesterol acyltransferase inhibitor 58-035 on foam cell development in primary human monocyte-derived macrophages. Rodriguez A, Bachorik PS, and Wee SB Arterioscler. Thromb. Vasc. Biol. 19(9), 2199-206, (1999)
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