SML1837

K-604

≥98% (HPLC)

• Synonym(e): 2-[4-[2-(Benzimidazol-2-ylthio)ethyl]piperazin-1yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide dihydrochloride, 4-[2-(1H-Benzimidazol-2-ylthio)ethyl]-N-[6-methyl-2,4-bis(methylthio)-3-pyridinyl]-1-piperazineacetamide dihydrochloride, K604
• Empirische Formel (Hill-System): C₂₃H₃₀N₆OS₃ · 2HCl
• CAS-Nummer: 217094-32-1
• Molekulargewicht: 575.64
• UNSPSC Code: 41106500
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Storage condition: desiccated

Eigenschaften

• Quality Segment: 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

Beschreibung

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..

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable