1. Apoptosis Autophagy Anti-infection Metabolic Enzyme/Protease
  2. Apoptosis Autophagy Bacterial Endogenous Metabolite
  3. Isoalantolactone

Isoalantolactone  (Synonyms: 异土木香内酯; (+)-Isoalantolactone; Isohelenin)

目录号: HY-N0780 纯度: 99.99%
COA 产品使用指南

Isoalantolactone 是一种烷化剂,用作细胞凋亡 (apoptosis) 诱导剂。

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Isoalantolactone Chemical Structure

Isoalantolactone Chemical Structure

CAS No. : 470-17-7

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10 mM * 1 mL in DMSO ¥715
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5 mg ¥406
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10 mg ¥650
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Customer Review

Other Forms of Isoalantolactone:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.

IC50 & Target

Apoptosis[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.38 μg/mL
Compound: 8
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
HeLa IC50
8.15 μM
Compound: Isoalantolactone
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 31784199]
HepG2 IC50
1.77 μg/mL
Compound: 8
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
HT-1080 IC50
0.795 μg/mL
Compound: 8
Antiproliferative activity against human HT1080 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human HT1080 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
HUVEC IC50
2.5 μg/mL
Compound: 8
Antiproliferative activity against human HUVEC assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
Antiproliferative activity against human HUVEC assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
[PMID: 23451797]
Platelet IC50
> 516.5 μM
Compound: Isoalantolactone
Antimigraine activity in bovine citreated platelet assessed as inhibition of [14C]serotonin release after 6 mins by scintillation counting
Antimigraine activity in bovine citreated platelet assessed as inhibition of [14C]serotonin release after 6 mins by scintillation counting
[PMID: 1431933]
体外研究
(In Vitro)

Isoalantolactone 对 K562 人白血病细胞系具有良好的细胞毒性 (IC50=1.2 μM)[1]。使用 PANC-1、BxPC3 和 HPAC 细胞系评估 Isoalantolactone 对胰腺癌的细胞毒性作用。用 Isoalantolactone 处理 24 小时以剂量依赖性方式抑制 PANC-1 细胞生长。在 80 μM 时抑制率超过 90%,达到 50% 生长抑制的浓度 (IC50) 为 40 μM。在 Isoalantolactone 处理的 BxPC3 和 HPAC 细胞中观察到类似的细胞活力丧失趋势,IC50 值分别为 43 和 48 μM。用 3 mM N-乙酰半胱氨酸 (NAC)? (一种特定的 ROS 清除剂) 预处理可恢复细胞的活力,这表明 Isoalantolactone 通过 ROS 的产生对细胞活力发挥细胞毒性作用[2]

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

体内研究
(In Vivo)

与对照组相比,Isoalantolactone 对 CD1 小鼠的急性和慢性毒性作用通过测量体重、血液生化和肝肾组织病理学的变化来评估。小鼠对异胡桃内酯具有良好的耐受性,并且在两个实验期间 (7 天和 30 天) 期间,在 100 mg/kg 的剂量下未发现死亡率或任何药毒性迹象。在两个实验期间,对照和处理小鼠的体重增加和食物消耗是可比较的,并且组织病理学和血液生化参数没有药物相关的变化。使用苏木精和伊红染色评估肝脏和肾脏的组织病理学变化,并与肝肾功能生物标志物相关联。对照组和处理组肝肾结构未见明显形态学改变。给药第7天处理组血清谷丙转氨酶 (ALT) 和天冬氨酸转氨酶 (AST) 水平略有升高,但与对照组无显著差异 (P<0.05)。在给药第 7 天,处理组总胆红素 (TBIL) 浓度显著增加 (1.43±0.26 vs 对照组 0.76±0.12,P<0.05)。同样,肾功能生物标志物的变化也没有显著差异 (P<0.05) ) 在剂量第 7 天时对照组和处理组的血清中。肌酐 (Cr) 的浓度略有增加,而处理组的血尿素氮 (BUN) 的浓度略有降低。给小鼠注射异胡桃内酯100 mg/kg 30天,血清AST、ALT、TBIL和BUN水平略有下降[2]

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

分子量

232.32

Formula

C15H20O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

异土木香内酯;异阿兰内酯

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 (430.44 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 4.3044 mL 21.5220 mL 43.0441 mL
5 mM 0.8609 mL 4.3044 mL 8.6088 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 (10.76 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。

    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 (10.76 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。

    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。
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)。
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: 99.99%

参考文献
Cell Assay
[2]

Cell viability is assessed by MTT assay. Briefly PANC-1, BxPC3, and HPAC cells are treated with DMSO or Isoalantolactone (5, 10, 20, 40, 80 and 100 μM) in the presence or absence of 3 mM NAC for 24 h. Following treatment, the MTT reagent is added (500 µg/mL) and cells are further incubated at 37°C for 4 h. Subsequently 150 μL DMSO is added to dissolve farmazan crystals and absorbance is measured at 570 nm in a microplate reader. The percentage of cell viability is calculated[2].

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

Animal Administration
[2]

Mice[2]
In vivo studies for acute and chronic toxicity are conducted on 10-12 week old CD1 mice weighing 27-30 g. The mice are maintained in a specific pathogen-free grade animal facility on a 12-h light/dark cycles at 25±2°C. Mice are randomly divided into four groups. Group A (n=4) administered with 50 µL DMSO intraperitonially for 7 days; Group B (n=4) administered with Isoalantolactone (100 mg/kg body weight) in 50 µL DMSO intraperitonially for 7 days; Group C (n=4) administered with 50 µL DMSO for 30 days and Group D (n=4) administered with Isoalantolactone (100 mg/kg body weight) in 50 µL DMSO intraperitonially for 30 days. At the first and last day of the experiments, the body weight of each mouse is measured. At the end of experiments (at dose day 7 for acute toxicity & dose day 30 for chronic toxicity), mice are anesthetized using Pentobarbital sodium (50 mg/kg ip), blood is collected via cardiac puncture, allowed to clot for 10 min and centrifuge at 1000×g for 10 min at room temperature. Serum is separated and stored at -20°C until analysis. The liver and kidneys are excised and processed for hematoxylin and eosin staining followed established procedures.

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, 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 4.3044 mL 21.5220 mL 43.0441 mL 107.6102 mL
5 mM 0.8609 mL 4.3044 mL 8.6088 mL 21.5220 mL
10 mM 0.4304 mL 2.1522 mL 4.3044 mL 10.7610 mL
15 mM 0.2870 mL 1.4348 mL 2.8696 mL 7.1740 mL
20 mM 0.2152 mL 1.0761 mL 2.1522 mL 5.3805 mL
25 mM 0.1722 mL 0.8609 mL 1.7218 mL 4.3044 mL
30 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
40 mM 0.1076 mL 0.5381 mL 1.0761 mL 2.6903 mL
50 mM 0.0861 mL 0.4304 mL 0.8609 mL 2.1522 mL
60 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
80 mM 0.0538 mL 0.2690 mL 0.5381 mL 1.3451 mL
100 mM 0.0430 mL 0.2152 mL 0.4304 mL 1.0761 mL
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产品名称:
Isoalantolactone
目录号:
HY-N0780
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