K-604 dihydrochloride|cas:217094-32-1|西域试剂

K-604 dihydrochloride,99.0%

产品编号：Bellancom-100400A| CAS NO：217094-32-1| 分子式：C₂₃H₃₂Cl₂N₆OS₃| 分子量：575.64

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100400A	￥1500.00	杭州北京（现货）
Bellancom-100400A	￥2400.00	杭州北京（现货）
Bellancom-100400A	￥4800.00	杭州北京（现货）
Bellancom-100400A	￥7500.00	杭州北京（现货）
Bellancom-100400A	￥11500.00	杭州北京（现货）

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K-604 dihydrochloride

产品介绍

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。

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.

体外研究

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 K_i value of 0.378 μM. K-604 efficiently inhibits cholesterol esterification in human macrophages with IC₅₀ value of 68 nM. 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.

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

体内研究

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.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (173.72 mM; Need ultrasonic)

DMSO : 62.5 mg/mL (108.57 mM; Need ultrasonic)

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
10 mM	0.1737 mL	0.8686 mL	1.7372 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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

1.

请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (173.72 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

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); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.91 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

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); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.91 mM，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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.25 mg/mL (3.91 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (3.91 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。