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Literature summary 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

EC Number Inhibitors Comment Organism Structure
2.3.1.26 (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
2.3.1.26 (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
2.3.1.26 (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
2.3.1.26 (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
2.3.1.26 pactimibe
-
 Oryctolagus cuniculus

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.26 Oryctolagus cuniculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.26 liver
-
 Oryctolagus cuniculus
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.3.1.26 ACAT
-
 Oryctolagus cuniculus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.26 37
-
 assay at Oryctolagus cuniculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.26 7.4
-
 assay at Oryctolagus cuniculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.26 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
2.3.1.26 0.000312
-
 pH 7.4, 37°C Oryctolagus cuniculus pactimibe