2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. K-604 dihydrochloride

K-604 dihydrochloride 

目录号: HY-100400A 纯度: ≥99.0%
COA 产品使用指南

摩尔计算器

K-604 dihydrochloride 是一种有效的选择性酰基辅酶 A：胆固醇酰基转移酶 1 (ACAT-1) 抑制剂，IC50 为 0.45±0.06 μM。

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K-604 dihydrochloride Chemical Structure

K-604 dihydrochloride Chemical Structure

CAS No. : 217094-32-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2090
In-stock
1 mg ￥681
In-stock
5 mg ￥1500
In-stock
10 mg ￥2400
In-stock
25 mg ￥4800
In-stock
50 mg ￥7500
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

K-604 dihydrochloride 相关抗体

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ACAT1 ACAT2 MGAT2 ACAT

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target[1]

ACAT-1

0.45 μM (IC50)

ACAT-2

102.85 μM (IC50)

体外研究
(In Vitro)

The potency and selectivity of K-604 for human ACAT-1 and ACAT-2 is examined. The IC50 value of K-604 for human ACAT-1 is 0.45 μM and that for human ACAT-2 is 102.85 μM, indicating that K-604 is 229-fold more selective for ACAT-1 than ACAT-2. Kinetic analysis indicates that the inhibition is competitive with respect to oleoyl-coenzyme A with a Ki value of 0.378 μM. K-604 efficiently inhibits cholesterol esterification in human macrophages with IC50 value of 68 nM[1]. In cell free biochemical assays, K604 at 0.5 µM inhibits ACAT1 enzymatic activity by 70% without significantly inhibiting the ACAT2 enzyme activity. To investigate whether blocking ACAT1 increases autophagy in neuronal cells, N2a cells are treated with K604. The result shows that at 0.1 to 1 µM, K604 inhibits ACAT activity by 60-80%. Next K604 is added to N2a cells at concentrations from 0.1 to 1 µM for 24 h, and LC3 levels are examined by western blot. The result shows that K604 increases the LC3-II/LC3-I ratio, a reliable marker for autophagosome formation, in a dose-dependent manner. The number of the fluorescent LC3 puncta is significantly increased in N2a cells after K604 treatment. By western blot, K604 significantly decreases the levels of p62 in N2a cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

K-604 dihydrochloride 相关抗体:
体内研究
(In Vivo)

Using F1B hamsters, an animal model susceptible to diet-induced hyperlipidemia and atherosclerosis, the effects of K-604 on aortic lesion areas and plasma cholesterol levels are assessed. Administration of K-604 does not affect body weight or food consumption. 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. Further, the histological analyses of the atherosclerotic lesions are performed. The fatty streak lesions in the control group are characterized by accumulation of foamy macrophages in the subendothelial space. In contrast, the areas occupied by foamy macrophages are markedly reduced by administration of K-604[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

575.64

Formula

C23H32Cl2N6OS3
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 100 mg/mL (173.72 mM; 超声助溶)

DMSO 中的溶解度 : 62.5 mg/mL (108.57 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7372 mL 8.6860 mL 17.3720 mL
5 mM 0.3474 mL 1.7372 mL 3.4744 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.25 mg/mL (3.91 mM); 澄清溶液

    此方案可获得 ≥ 2.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.25 mg/mL (3.91 mM); 澄清溶液

    此方案可获得 ≥ 2.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂： PBS

    Solubility: 100 mg/mL (173.72 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥99.0%

COA (171 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

ACAT activity is determined by measuring the production of cholesteryl[14C]oleate. Microsomal fractions derived from CHO-ACAT-1 or CHO-ACAT-2 cells are diluted with CHAPS in 0.5 M KCl, 0.5 mM EDTA, and 25 mM Tris-HCl (pH 7.8) (buffer A) to a final protein concentration of 1.0 mg/mL. The microsomal fractions containing 9.2 μg of protein for ACAT-1 or 4.9 μg for ACAT-2 in 10 μL of buffer A are mixed with various concentrations of K-604 (0.4, 0.6 and 0.8 μM) or CI-1011 in 5 μL of DMSO, and reconstituted with 152.5 μL of mixed micelles containing 1.6 mM Cholesterol, 11.2 mM Phosphatidylcholine, and 9.3 mM Taurocholate in 25, 0.5 mM EDTA, and Tris-HCl (pH 7.8). The reaction is started by adding 10 μL of 0.45 μM [14C]oleoyl-CoA, 10 nM fatty acid-free bovine serum albumin (fatty acid-free BSA) and 25 mM Tris-HCl (pH 7.8). Reaction mixtures are incubated for 25 min at 37°C and terminated by adding 150 μL of Chloroform/Methanol (2:1). The organic phase is dried under a stream of nitrogen. The lipids are resuspended with 150 μL of Chloroform/Methanol (2:1) and developed by thin layer chromatography (TLC) using hexane/diethyl ether/acetic acid (75:25:1). Radioactivities of cholesterol [14C]oleate are determined using a BAS 2500 image analyzer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

The mouse neuroblastoma cell line N2a is cultured in DMEM/Opti-MEM (50:50) with 10% fetal bovine serum (FBS) at 37°C with 5% CO2 in a humidified incubator. Cells are incubated for 24 h with the ACAT1-specific inhibitor K604 (0.1, 0.5 and 1 µM) or isotype-nonspecific ACAT inhibitor CI-1011. Primary cortical neurons are isolated from mouse brains at postnatal day 0-3. Cortical neurons are plated in 6 well plates at 350,000 cells/well and grown in 2 mL/well Neurobasal A with 1×B27, 0.5 mM L-glutamine, and 5 ng/mL fibroblast growth factor. Half of the media is replaced with fresh media once every 7 days. After 14-21 days in culture, cells are used for individual experiments[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Hamsters[1]
Male F1B hamsters (n=30) at 8 weeks old are used for animal experiments. The animal room is controlled at 23±3°C and relative humidity of 50±20%. Animals are fed a CE-2 chow diet, followed by supplementation with CE-2 containing 0.3% cholesterol and 10% coconut oil for 10 weeks. During fat loading, K-604 is administered orally at 1, 3, 10, or 30 mg/kg/day (n=6 for each dose group). The control group (n=6) receive an aqueous solution of 0.5% methylcellulose instead of K-604. Tap water is given ad libitum. Body weight is measured at the time of drug administration. Blood is sampled for determination of plasma cholesterol levels using a commercially available kit (Cholesterol E-Test).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

K-604 dihydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.7372 mL 8.6860 mL 17.3720 mL 43.4299 mL
5 mM 0.3474 mL 1.7372 mL 3.4744 mL 8.6860 mL
10 mM 0.1737 mL 0.8686 mL 1.7372 mL 4.3430 mL
15 mM 0.1158 mL 0.5791 mL 1.1581 mL 2.8953 mL
20 mM 0.0869 mL 0.4343 mL 0.8686 mL 2.1715 mL
25 mM 0.0695 mL 0.3474 mL 0.6949 mL 1.7372 mL
30 mM 0.0579 mL 0.2895 mL 0.5791 mL 1.4477 mL
40 mM 0.0434 mL 0.2171 mL 0.4343 mL 1.0857 mL
50 mM 0.0347 mL 0.1737 mL 0.3474 mL 0.8686 mL
60 mM 0.0290 mL 0.1448 mL 0.2895 mL 0.7238 mL
80 mM 0.0217 mL 0.1086 mL 0.2171 mL 0.5429 mL
100 mM 0.0174 mL 0.0869 mL 0.1737 mL 0.4343 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K-604217094-32-1K604K 604AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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