2. Autophagy Membrane Transporter/Ion Channel
  3. Autophagy Potassium Channel
  4. Daurisoline

Daurisoline  (Synonyms: 蝙蝠葛苏林碱; (R,R)-Daurisoline)

目录号: HY-N0221 纯度: 99.67%
COA 产品使用指南

摩尔计算器

Daurisoline 是一种，可从蝙蝠葛 (Menispermum dauricum) 和北豆根 (Rhizoma Menispermi) 中分离得到的双苄基异喹啉生物碱。Daurisoline 对 hERG 具有阻断作用，具有抗心律失常作用。Daurisoline 是一种有效的自噬阻断剂，可用于癌症研究。

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Daurisoline Chemical Structure

Daurisoline Chemical Structure

CAS No. : 70553-76-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1035
In-stock
5 mg ￥770
In-stock
10 mg ￥1350
In-stock
25 mg ￥2850
In-stock
50 mg ￥5200
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Daurisoline:

Daurisoline 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer[1][2].

IC50 & Target

hERG[1], autophagy[2]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A673 GI50
9.2 μM
Compound: 17
Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HCC1806 GI50
17 μM
Compound: 17
Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HCC1937 GI50
6.9 μM
Compound: 17
Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HCC70 GI50
8.8 μM
Compound: 17
Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
HEK293 IC50
9.1 μM
Compound: 1
Inhibition of human ERG stepped current expressed in HEK293 cells at + 20 mV holding potential by patch clamp assay
Inhibition of human ERG stepped current expressed in HEK293 cells at + 20 mV holding potential by patch clamp assay
[PMID: 22974355]
HEK293 IC50
9.6 μM
Compound: 1
Inhibition of human ERG tail current expressed in HEK293 cells at + 60 mV holding potential by patch clamp assay
Inhibition of human ERG tail current expressed in HEK293 cells at + 60 mV holding potential by patch clamp assay
[PMID: 22974355]
MDA-MB-231 GI50
13 μM
Compound: 17
Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
MDA-MB-453 GI50
9 μM
Compound: 17
Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
SJRH30 GI50
3.7 μM
Compound: 17
Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
[PMID: 33226219]
体外研究
(In Vitro)

Daurisoline（compound 1）在 +20 mV 时对去极化末期（IhERG-step）有最大抑制作用，在 +60 mV 时对峰值尾电流（IhERG-tail）有最大抑制作用。 在浓度为 1、3、10 和 30 μM 时，去极化末期（IhERG-step）电流幅度的抑制率分别为 32.2±4.2%、41.6±2.6%、62.1±5.9% 和 74.8±6.8%；IC50 为 9.1 μM。 而IhERG-tail的抑制率分别为16.7±5.8%、31.1±4.5%、55.1±7.2%和81.2±7.0%，IC50为9.6 μM[1]。
Daurisoline (DAS)抑制不同癌细胞系中CPT诱导的自噬，在HeLa、A549和HCT-116细胞中的IC50分别为74.75±1.03、50.54±1.02和80.81±1.10 μM。 DAC 和 Daurisoline 还通过抑制 DAC 和 Daurisoline 处理的细胞中的溶酶体 V 型 ATPase 活性来损害溶酶体功能和溶酶体酸化[2]。

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

Daurisoline 相关抗体:
体内研究
(In Vivo)

静脉注射 Daurisoline (DS) 或 dauricine (Dau) 6 mg/kg 后，血浆浓度呈双指数下降。比格犬静脉注射 Daurisoline 和 Dau 6 mg/kg 后，HR、LVSP、dp/dtmax 和 SBP 均降低。但观察到两种药物的最大药理作用峰值均晚于最大血药浓度10-15分钟[3]。

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

610.74

Formula

C37H42N2O6
CAS 号
性状

固体

颜色

White to off-white

中文名称

蝙蝠葛苏林碱
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (163.74 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 1.6374 mL 8.1868 mL 16.3736 mL
5 mM 0.3275 mL 1.6374 mL 3.2747 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。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.09 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (4.09 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。

以下溶解方案，请直接配制工作液。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： 50% PEG300    50% Saline

    Solubility: 20 mg/mL (32.75 mM); 澄清溶液; 超声助溶

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
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）。
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: 99.67%

COA (286 KB) LCMS (86 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[2]

HEK293 cells are incubated overnight with 35 μg/mL Dx-OG514. Cells are washed and incubated with serum-free Dulbecco's modified Eagle's medium (DMEM) for 2 h. 15 minutes prior to lysis, FCCP is added into the medium to a final concentration of 1 μM. Cells are scraped in fraction buffer (50 mM KCl, 90 mM K-Gluconate, 1 mM EGTA, 50 mM Glucose, 20 mM HEPES, protease inhibitor cocktail, pH=7.4) supplemented with 1 μM FCCP. After spraying with needle, cells are spun down at 10,000 rpm for 15 sec. at 4°C. Then, re-centrifuge the supernatant at max speed for another 20 minutes. The pellet is resuspended in pre-warmed fractionation buffer supplemented with 1% BSA, and split into several aliquots with DAC, Daurisoline (DAS) or BAF treatment for 30 min. Baseline fluorescence is measured at 530 nm upon 511 nm excitation in 96-well plate at 30 s intervals for 5 min[2].

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

Cell proliferation is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. HeLa cells are seeded at 7000 cells per well in 96-well plates in DMEM (1% serum). After cells are treated with different compounds (including Daurisoline) for indicated times, 20 μL of MTT (2.5 mg/mL in PBS) is added to each well. The plates are incubated for an additional 4 h at 37°C. Then the purple-blue MTT formazan precipitate is dissolved in 100 μL DMSO. The cell viability of HeLa cell is evaluated by measuring optical density at 572 nm with a microplate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

After the beagle dogs are anesthetized with sodium pentobarbital (30 mg/kg, iv) a canula is advanced into the left ventricle through the right common carotid artery. And the canula is connected to a pressure transducer which is connected to an amplifier and polygraph. The right femoral artery is canulated to measure the blood pressure wave. ECG (lead II) is observed simultaneously. After iv injection of Daurisoline (DS) (n=4) or Dau (n=4) to beagle dogs, the ECG, BP, and LVP signals are recorded. Blood samples are taken before dosing and at 2, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 6, 8 h after dosing[3].

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

Daurisoline 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。-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 1 mM 1.6374 mL 8.1868 mL 16.3736 mL 40.9339 mL
5 mM 0.3275 mL 1.6374 mL 3.2747 mL 8.1868 mL
10 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0934 mL
15 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7289 mL
20 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
25 mM 0.0655 mL 0.3275 mL 0.6549 mL 1.6374 mL
30 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3645 mL
40 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0233 mL
50 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
60 mM 0.0273 mL 0.1364 mL 0.2729 mL 0.6822 mL
80 mM 0.0205 mL 0.1023 mL 0.2047 mL 0.5117 mL
100 mM 0.0164 mL 0.0819 mL 0.1637 mL 0.4093 mL
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:

Daurisoline70553-76-3(R,R)-Daurisoline蝙蝠葛苏林碱AutophagyPotassium ChannelKcsAantiarrhythmicalkaloidMenispermum dauricumRhizoma MenispermiInhibitorinhibitorinhibit

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