K-604 (hydrochloride)

K-604 is an inhibitor of acyl-coenzyme A:cholesterol acyltransferase-1 (ACAT-1, IC50 = 0.45 µM). It is selective for ACAT-1 over ACAT-2 (IC50 = 102.85 µM). K-604 reduces foaming of J774 macrophages (IC50 = 0.026 µM) and reduces cholesterol esterification in monocyte-derived macrophages (IC50 = 0.068 µM). It decreases lipid-accumulation areas in the aortic arch in atherosclerosis-susceptible Bio F1B hamsters fed a high-fat and high-cholesterol diet when administered at a dose of 10 mg/kg and reduces plasma total cholesterol levels in the same model at 10 and 30 mg/kg. K-604 also increases the LC3-II-to-LC3-I ratio, a marker of autophagosome formation, in Neuro2a (N2a) mouse neuroblastoma cells when used at concentrations of 0.1 and 1 µM. It decreases wild-type and mutant P301L-tau levels in N2a cells overexpressing these proteins but does not affect endogenous tau levels. Intranasal administration of K-604 (105 µg/animal) reduces the level of brain cholesteryl esters in mice.Formal Name: 4-[2-(1H-benzimidazol-2-ylthio)ethyl]-N-[6-methyl-2,4-bis(methylthio)-3-pyridinyl]-1-piperazineacetamide, dihydrochloride. CAS Number: 217094-32-1. Molecular Formula: C23H30N6OS3 . 2HCl. Formula Weight: 575.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml. SMILES: O=C(CN1CCN(CC1)CCSC2=NC3=CC=CC=C3N2)NC4=C(SC)N=C(C)C=C4SC.Cl.Cl. InChi Code: InChI=1S/C23H30N6OS3.2ClH/c1-16-14-19(31-2)21(22(24-16)32-3)27-20(30)15-29-10-8-28(9-11-29)12-13-33-23-25-17-6-4-5-7-18(17)26-23,,/h4-7,14H,8-13,15H2,1-3H3,(H,25,26)(H,27,30),2*1H. InChi Key: DEKWEGUBUYKTAV-UHFFFAOYSA-N.