产品说明书

K-604 2HCl

Print
Chemical Structure| 217094-32-1 同义名 : K-604 dihydrochloride
CAS号 : 217094-32-1
货号 : A1251721
分子式 : C23H32Cl2N6OS3
纯度 : 98%
分子量 : 575.641
MDL号 : MFCD30738203
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(104.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(173.72 mM)，配合低频超声助溶
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.69mL

1.74mL

0.87mL

17.37mL

3.47mL

1.74mL
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.