SML1837

Sigma-Aldrich

K-604

≥98% (HPLC)

Sinónimos:
2-4-2-(Benzimidazol-2-ylthio)ethylpiperazin-1yl-N-2,4-bis(methylthio)-6-methyl-3-pyridylacetamide dihydrochloride, 4-2-(1H-Benzimidazol-2-ylthio)ethyl-N-6-methyl-2,4-bis(methylthio)-3-pyridinyl-1-piperazineacetamide dihydrochloride, K604
Empirical Formula (Hill Notation):
C23H30N6OS3 · 2HCl
Número de CAS:
Peso molecular:
575.64
En este momento no podemos mostrarle ni los precios ni la disponibilidad

Quality Level

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.HCl.HCl

Packaging

5, 25 mg in glass bottle

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).

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point F

Not applicable

Flash Point C

Not applicable

Yohei Shibuya et al.
Neurobiology of aging, 36(7), 2248-2259 (2015-05-02)
Patients with Alzheimer's disease (AD) display amyloidopathy and tauopathy. In mouse models of AD, pharmacological inhibition using small molecule enzyme inhibitors or genetic inactivation of acyl-coenzyme A (Acyl-CoA):cholesterol acyltransferase 1 (ACAT1) diminished amyloidopathy and restored cognitive deficits. In microglia, ACAT1...
Mami Ikenoya et al.
Atherosclerosis, 191(2), 290-297 (2006-07-06)
Acyl-coenzyme A:cholesterol O-acyltransferase-1 (ACAT-1), a major ACAT isozyme in macrophages, plays an essential role in foam cell formation in atherosclerotic lesions. However, whether pharmacological inhibition of macrophage ACAT-1 causes exacerbation or suppression of atherosclerosis is controversial. We developed and characterized...
Yasunobu Yoshinaka et al.
Atherosclerosis, 213(1), 85-91 (2010-09-17)
Acyl-coenzyme A:cholesterol O-acyltransferase-1 (ACAT-1) plays an essential role in macrophage foam cell formation and progression of atherosclerosis. We developed a potent and selective ACAT-1 inhibitor, K-604, and tested its effects in apoE-knockout mice. Administration of K-604 to 8-week-old apoE-knockout mice...
Rik van der Kant et al.
Cell stem cell, 24(3), 363-375 (2019-01-29)
Genetic, epidemiologic, and biochemical evidence suggests that predisposition to Alzheimer's disease (AD) may arise from altered cholesterol metabolism, although the molecular pathways that may link cholesterol to AD phenotypes are only partially understood. Here, we perform a phenotypic screen for...

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