|2-(4-(2-((1H-苯并[d]咪唑-2-基)硫代)乙基)哌嗪-1-基)-N-(6-甲基-2,4-双(甲硫基)吡啶-3-基)乙酰胺二盐酸盐|CsnPharm

CAS No.: 217094-32-1

K-604 2HCl Catalog No. CSN27700

Synonyms: K-604 HCl;K-604 Hydrochloride;K-604

K-604 is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor. 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.

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技术信息

生物活性

描述Acetyl-CoA acetyltransferase 1 (ACAT 1) is a protein coding gene that encodes a nitochondrially localized enzyme that catalyzes the reversible formation of acetoacetyl-CoA rom two molecules of acetyl-CoA. This enzyme plays an essential role in breaking down proteins and fats from diet. it helps process isoleucine, an amino acid that is a building block of many proteins. This enzyme is also involved in processing ketones, which are molecules that are produced when fats are broken down in the body. K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM. K-604 efficiently inhibits cholesterol esterification in human macrophages with IC50 value of 68 nM. The plasma cholesterol levels in fat-fed hamsters are ~12-fold higher than those in chow-fed hamsters, which are significantly decreased by K-604 only at the highest dose tested (30 mg/kg) but not at lower doses (1-10 mg/kg). The fatty streak lesions stain with oil red O are markedly induced by the high-fat diet, which is significantly reduced by administration of K-604.^[1]. Administration of K-604 to 8-week-old apoE-knockout mice for 12 weeks at a dose of 60 mg/kg/day significantly reduced macrophage-positive area and increased collagen-positive area in atherosclerotic plaques in the aorta without affecting plasma cholesterol levels or lesion areas, indicating direct plaque-modulating effects of K-604 on vascular walls independent of plasma cholesterol levels. Exposure of cultured human aortic smooth muscle cells to K-604 resulted in increased procollagen type 1 contents in the culture supernatant and increased procollagen type 1 mRNA levels^[2].
参考文献

[1] Ikenoya M, et al. A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007. 191(2), 290-7.
[2] Yoshinaka, Y., Shibata, H. et al. A selective ACAT-1 in hibitor, K-604, stimulates collagen production in cultured smooth muscle cells and alters plaque phenotype in apolipoprotein E-knockout mice. ELSEVIER. 2010. 213 (1), 85-91.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7372 mL
- 8.6860 mL
- 17.3719 mL
- 5 mM
- 0.3474 mL
- 1.7372 mL
- 3.4744 mL
- 10 mM
- 0.1737 mL
- 0.8686 mL
- 1.7372 mL

技术信息

CAS号	217094-32-1	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C23H32Cl2N6OS3	运输	蓝冰
分子量	575.64	别名	K-604 HCl;K-604 Hydrochloride;K-604

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