Coptisine chloride - CAS:6020-18-4

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Coptisine chloride (Synonyms:盐酸黄连碱)

目录号 : KM19053 CAS No. : 6020-18-4 纯度 : 98%

Data Sheet 产品使用指南

Coptisine chloride 是从黄连中分离到的生物碱，是一种有效的非竞争性的 IDO 抑制剂，K_i 值为 5.8 μM，IC₅₀ 值为 6.3 μM。Coptisine chloride 是一种有效的 H1N1 神经氨酸酶 (NA-1) 抑制剂，IC₅₀ 为 104.6 μg/mL，可用于甲型流感病毒 (H1N1) 感染。

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5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a K_i value of 5.8 μM and an IC₅₀ value of 6.3 μM. Coptisine chloride is a potent H1N1 neuraminidase (NA-1) inhibitor with an IC₅₀ of 104.6 μg/mL and can be used for influenza A (H1N1) infection.

体外研究

Coptisine chloride is an efficient uncompetitive IDO inhibitor with a K_i value of 5.8 μM and an IC₅₀ value of 6.3 μM. Coptisine (0.1-100 μM) inhibits the proliferation of A549, H460, H2170, MDA-MB-231 and HT-29 cells, with IC₅₀s of 18.09, 29.50, 21.60, 20.15 and 26.60 µM, respectively. Coptisine (12.5, 25, 50 μM) upregulates the expression of pH2AX and p21, reduces expression of cyclin B1, cdc2, and cdc25C, and induces G2/M arrest and apoptosis of A549 cells in a concentration-dependent manner. Coptisine (12.5, 25, 50 μM) also induces mitochondrial dysfunction and activates caspases activities in A549 cells. Furthermore, Coptisine (50 μM) increases ROS levels in a time-dependent manner (0.5, 1, 2, 4, 12, and 24 h).

体内研究

Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD₅₀ value of 880.18 mg/kg. Coptisine (154 mg/kg/day, 90 days) shows no toxicity on SD rats. Coptisine (23.35, 46.7, 70.05 mg/kg, p.o.) dose-dependently decreases the levels of TC, TG, and LDL-c and increases HDL-c content in serum of hamsters to different degree, slows down weight gain induced by the HFHC diet, and raises the level of cholesterol and TBA in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR protein expression level and induces the protein expression of SREBP-2, LDLR, and CYP7A1 involved in cholesterol metabolism.

分子式

C₁₉H₁₄ClNO₄

分子量

355.77

CAS号

6020-18-4

中文名称

盐酸黄连碱；氯化黄连碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 10.42 mg/mL (29.29 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8108 mL	14.0540 mL	28.1080 mL
5 mM	0.5622 mL	2.8108 mL	5.6216 mL
10 mM	0.2811 mL	1.4054 mL	2.8108 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。-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： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.04 mg/mL (2.92 mM); Clear solution

此方案可获得 ≥ 1.04 mg/mL (2.92 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.4 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。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.5 mg/mL (1.41 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 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。