1. Metabolic Enzyme/Protease Anti-infection
  2. Indoleamine 2,3-Dioxygenase (IDO) Bacterial Influenza Virus
  3. Coptisine chloride

Coptisine chloride  (Synonyms: 盐酸黄连碱)

目录号: HY-N0736 纯度: 99.73%
COA 产品使用指南 技术支持

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,Ki 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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Coptisine chloride Chemical Structure

Coptisine chloride Chemical Structure

CAS No. : 6020-18-4

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10 mM * 1 mL in DMSO ¥587
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1 mg ¥333
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5 mg ¥750
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10 mg ¥1200
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25 mg ¥2400
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Customer Review

Other Forms of Coptisine chloride:

查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki 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.

IC50 & Target[1]

IDO

6.3 μM (IC50)

IDO

5.8 μM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A10 GI50
4.49 μM
Compound: 1
Growth inhibition against rat A10 cells after 72 hrs by MTT assay
Growth inhibition against rat A10 cells after 72 hrs by MTT assay
[PMID: 21401114]
A549 IC50
> 14.05 μM
Compound: 1
Cytotoxicity against human A549 cells assessed as growth inhibition rate after 96 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as growth inhibition rate after 96 hrs by MTT assay
[PMID: 25203783]
A549 IC50
23.96 μM
Compound: 7
Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
[PMID: 20594848]
Bel-7402 IC50
> 14.05 μM
Compound: 1
Cytotoxicity against human Bel7402 cells assessed as growth inhibition rate after 96 hrs by MTT assay
Cytotoxicity against human Bel7402 cells assessed as growth inhibition rate after 96 hrs by MTT assay
[PMID: 25203783]
C-33-A IC50
> 14.05 μM
Compound: 1
Cytotoxicity against human C33A cells assessed as growth inhibition rate after 96 hrs by MTT assay
Cytotoxicity against human C33A cells assessed as growth inhibition rate after 96 hrs by MTT assay
[PMID: 25203783]
G-402 GI50
19.1 μM
Compound: 1
Growth inhibition against human G402 cells after 48 hrs by MTT assay
Growth inhibition against human G402 cells after 48 hrs by MTT assay
[PMID: 21401114]
HCT-15 IC50
29.07 μM
Compound: 7
Cytotoxicity against human HCT15 cells by SRB assay
Cytotoxicity against human HCT15 cells by SRB assay
[PMID: 20594848]
HCT-8 IC50
5.59 μM
Compound: 1
Cytotoxicity against human HCT8 cells assessed as growth inhibition rate after 96 hrs by MTT assay
Cytotoxicity against human HCT8 cells assessed as growth inhibition rate after 96 hrs by MTT assay
[PMID: 25203783]
SK-MEL-2 IC50
> 30 μM
Compound: 7
Cytotoxicity against human SK-MEL-2 cells by SRB assay
Cytotoxicity against human SK-MEL-2 cells by SRB assay
[PMID: 20594848]
SK-OV-3 IC50
> 30 μM
Compound: 7
Cytotoxicity against human SKOV3 cells by SRB assay
Cytotoxicity against human SKOV3 cells by SRB assay
[PMID: 20594848]
VSMC GI50
3.35 μM
Compound: 1
Growth inhibition against rat VSMC after 72 hrs by MTT assay
Growth inhibition against rat VSMC after 72 hrs by MTT assay
[PMID: 21401114]
体外研究
(In Vitro)

Coptisine chloride 是一种有效的非竞争性 IDO 抑制剂,Ki 值为 5.8 μM,IC50 值为 6.3 μM[1]。Coptisine (0.1-100 μM) 抑制 A549, H460, H2170, MDA-MB-231 和 HT-29 细胞增殖,IC50 分别为 18.09, 29.50, 21.60, 20.15 和 26.60 μM。Coptisine (12.5, 25, 50 μM) 上调 pH2AX 和 p21 表达,下调 cyclin B1, cdc2 和 cdc25C 表达,诱导 A549 细胞 G2/M 阶段阻滞和凋亡,并以浓度依赖性方式引起线粒体功能障碍和激活 caspase 活性[3]。同时,Coptisine (50 μM) 在 0.5, 1, 2, 4, 12 和 24 小时的时间范围内诱导活性氧水平升高[3]

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

体内研究
(In Vivo)

Coptisine 在小鼠中表现出浓度依赖性毒性,LD50 值为 880.18 mg/kg。Coptisine (154 mg/kg/day, 90 天) 对 SD 大鼠无毒性。Coptisine (23.35、46.7、70.05 mg/kg, p.o.) 剂量依赖性地降低了荷斯特的 TC、TG 和 LDL-c 水平,并不同程度地增加了血清中 HDL-c 含量,减缓了 HFHC 饮食引起的体重增加,并剂量依赖性地升高了荷斯特粪便中的胆固醇和 TBA 水平。Coptisine (70.05 mg/kg, p.o.) 抑制了 HMGCR 蛋白表达,诱导了与胆固醇代谢相关的 SREBP-2、LDLR 和 CYP7A1 蛋白的表达 [2]

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

分子量

355.77

Formula

C19H14ClNO4

CAS 号
性状

固体

颜色

Brown to orange

中文名称

盐酸黄连碱;氯化黄连碱

结构分类
初始来源
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 10.42 mg/mL (29.29 mM; 超声助溶 (<60°C); 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 2.8108 mL 14.0540 mL 28.1080 mL
5 mM 0.5622 mL 2.8108 mL 5.6216 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, 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。

  • 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

动物实验:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.04 mg/mL (2.92 mM); 澄清溶液

    此方案可获得 ≥ 1.04 mg/mL(饱和度未知)的澄清溶液。

    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 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。
  • 方案 二

    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); 澄清溶液

    此方案可获得 ≥ 0.5 mg/mL(饱和度未知)的澄清溶液。

    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;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。
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

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.73%

参考文献
Cell Assay
[3]

A 100-mM concentration of Coptisine is dissolved in DMSO, and subsequent concentrations ranging between 100 and 0.1 µM are prepared by diluting with cell culture medium. The final DMSO concentration used is less than 0.1% in every treatment. MTT assay is performed to assess cell proliferation effect of Coptisine. Briefly, 2500 cells/well are seeded in 96-well plate containing DMEM medium supplemented with 10% FBS and 1% penicillin-streptomycin. A series of Coptisine concentrations are added and incubated for 48 h in the presence or absence of 5-mM NAC. After 48 h of incubation, 15 µL of MTT (5 mg/mL) is added to each well and incubated at 37°C for 4 h. Then, the supernatant is removed and 150 µL of DMSO is added to each well to dissolve the crystals. The absorbance is measured at 595 nm by Spectramax M4 plate reader[3].

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

Animal Administration
[2]

Mice[2]
The acute toxicity of Coptisine is tested on Kunming mice, 10 mice in each group (half each males and females). Coptisine is dissolved in distilled water and prepared for administration with eight doses (482.5, 579, 694, 833, 1,000, 1,200, 1,440, and 1,728 mg/kg). After oral administration, the reactions of each mouse including mortality are observed and recorded for 1 week to obtain the LD50 value of Coptisine.
Rats[2]
Forty SD rats are divided into the control and Coptisine groups (half each males and females) which are treated for 90 days. The animal dose is calculated by the human equivalent dose (HED) with the body surface area (BSA) normalization method. To determine the sub-chronic toxicity, the actual dosage of Coptisine on SD rats (154 mg/kg/day) is obtained using the maximum HED of Coptisine (25 mg/kg) for an adult (60 kg) as a reference. Rats in the control group are given the same volume of 0.9 % saline. In the whole experiment, all animals are fed a normal diet and water ad libitum. The general appearance and behavior of rats are recorded daily, their body weight is measured every 10 days, and clinical signs and mortality are observed twice daily.

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

参考文献

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, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8108 mL 14.0540 mL 28.1080 mL 70.2701 mL
5 mM 0.5622 mL 2.8108 mL 5.6216 mL 14.0540 mL
10 mM 0.2811 mL 1.4054 mL 2.8108 mL 7.0270 mL
15 mM 0.1874 mL 0.9369 mL 1.8739 mL 4.6847 mL
20 mM 0.1405 mL 0.7027 mL 1.4054 mL 3.5135 mL
25 mM 0.1124 mL 0.5622 mL 1.1243 mL 2.8108 mL
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Coptisine chloride
目录号:
HY-N0736
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