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K-604 2HCl {[allProObj[0].p_purity_real_show]}

货号:A1251721 同义名: K-604 dihydrochloride

K-604 2HCl是一种高效选择性的乙酰辅酶 A:胆固醇酰基转移酶 1(ACAT-1)抑制剂。

K-604 2HCl 化学结构 CAS号:217094-32-1
K-604 2HCl 化学结构
CAS号:217094-32-1
K-604 2HCl 3D分子结构
CAS号:217094-32-1
K-604 2HCl 化学结构 CAS号:217094-32-1
K-604 2HCl 3D分子结构 CAS号:217094-32-1
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K-604 2HCl 纯度/质量文件 产品仅供科研

货号:A1251721 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Transferase 其他靶点 纯度
Tipifarnib +++

FTase, IC50: 0.6 nM

99%+
Tolcapone +

COMT, Ki: 30 nM

99%+
Lonafarnib +++

K-ras-4B, IC50: 2.8 nM

H-ras, IC50: 1.9 nM

99%+
(E)-Daporinad ++++

NMPRTase, Ki: 0.4 nM

99%+
FTI-277 HCl ++++

FTase, IC50: 500 pM

98%
A 922500 ++

mouse DGAT-1, IC50: 24 nM

human DGAT-1, IC50: 7 nM

98%
Lomeguatrib ++

O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM

99%+
PF-04620110 +

DGAT1, IC50: 19 nM

99%
LB42708 +++

FTase (K-Ras), IC50: 0.8 nM

FTase (N-ras), IC50: 1.2 nM

98%
GGTI298 Trifluoroacetate 98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

K-604 2HCl 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].

K-604 2HCl 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.

K-604 2HCl 实验方案

计算器
存储液制备 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

K-604 2HCl 技术信息

CAS号217094-32-1
分子式C23H32Cl2N6OS3
分子量 575.641
别名 K-604 dihydrochloride
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
动物实验配方
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