Biochem/physiol Actions
K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. 102.85 μ M against human ACAT1 and ACAT2, respectively) and acyl-CoA-competitive (Ki = 378 nM against oleoyl-coA) manner. K-604 inhibits cholesterol esterification in human monocyte-derived macrophages (IC50 = 68.0 nM) and enhances cholesterol efflux from THP-1 macrophages in response to HDL3 or apolipoprotein A-I. Oral administration is efficacious against macrophage foam cell formation and atherosclerosis progression among F1B hamsters on a high-fat diet (1-10 mg/kg/day) and apoE-knockout mice (60 mg/kg/day) without affecting plasma cholesterol levels. K-604 is also reported to stimulate autophagy-mediated P301L-Tau degradation in cortical neurons from 3XTg-AD mice (500 nM).
K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy..
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 10 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | O=C(NC1=C(SC)C=C(C)N=C1SC)CN2CCN(CCSC3=NC4=CC=CC=C4N3)CC2.[H]Cl.[H]Cl |
| InChI key | DEKWEGUBUYKTAV-UHFFFAOYSA-N |

