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Literature summary for 2.3.1.26 extracted from

  • Ohta, M.; Takahashi, K.; Kasai, M.; Shoji, Y.; Kunishiro, K.; Miike, T.; Kanda, M.; Mukai, C.; Shirahase, H.
    Novel tetrahydroisoquinoline derivatives with inhibitory activities against acyl-CoA: cholesterol acyltransferase and lipid peroxidation (2010), Chem. Pharm. Bull., 58, 1066-1076.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(S)-7-dimethylamino-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-isobutyryl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide shows about 16fold stronger anti-foam cell formation activity, 3fold stronger hepatic ACAT inhibitory activity, similar anti-low density lipoprotein (LDL) oxidative activity and 2fold more potent protective activity against macrophage cell death by oxidative stress in comparison with Pactimibe Oryctolagus cuniculus
(S)-N-(2,6-diisopropylphenyl)-2-octanoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide ratio IC50 of pactimibe/IC50 of test compound: 2.2 Oryctolagus cuniculus
(S)-N-(4-amino-2,6-diisopropylphenyl)-2-octanoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride ratio IC50 of pactimibe/IC50 of test compound: 0.96 Oryctolagus cuniculus
(S)-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-octanoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide ratio IC50 of pactimibe/IC50 of test compound: 10 Oryctolagus cuniculus
pactimibe
-
Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
oleoyl-CoA + cholesterol
-
Oryctolagus cuniculus CoA + cholesteryl oleate
-
?

Synonyms

Synonyms Comment Organism
ACAT
-
Oryctolagus cuniculus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Oryctolagus cuniculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Oryctolagus cuniculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000113
-
pH 7.4, 37°C Oryctolagus cuniculus (S)-7-dimethylamino-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-isobutyryl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
0.000312
-
pH 7.4, 37°C Oryctolagus cuniculus pactimibe