Nordihydroguaiaretic acid (Synonyms: 去甲二氢愈创木酸; NDGA)

目录号: HY-N0198 纯度: 99.93%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Nordihydroguaiaretic acid 是一种 5-脂氧合酶 (5LOX) (IC₅₀=8 μM) 和酪氨酸激酶抑制剂。

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Nordihydroguaiaretic acid Chemical Structure

CAS No. : 500-38-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥660	In-stock
100 mg	￥600	In-stock
250 mg	￥1200	In-stock
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1 g		询价

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Other Forms of Nordihydroguaiaretic acid:

Nordihydroguaiaretic acid (Standard) 询价

MCE 顾客使用本产品发表的 4 篇科研文献

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5-LOX 12-LOX 15-LOX

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC₅₀=8 μM) and tyrosine kinase inhibitor.

IC₅₀ & Target^[1]

5-LOX

8 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	54.3 μM Compound: NDGA	Cytotoxicity against human A375 cells after 5 days by MTT assay Cytotoxicity against human A375 cells after 5 days by MTT assay	[PMID: 19615898]
BGC-823	IC₅₀	> 60 μM Compound: NDGA	Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 27829519]
HEK293	EC₅₀	35 μM Compound: NDGA	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay	[PMID: 30878828]
HEK293	EC₅₀	4.9 μM Compound: NDGA	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Calcium-5 dye based fluorescence assay Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Calcium-5 dye based fluorescence assay	[PMID: 30878828]
HeLa	IC₅₀	0.08 μg/mL Compound: NDGA	Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA	[PMID: 19942440]
Hepatocyte	IC₅₀	3 x 10⁴ nM Compound: Nordihydroguaiaretic acid	Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs	[PMID: 18212104]
HepG2	IC₅₀	54.1 μM Compound: NDGA	Cytotoxicity against human HepG2 cells after 5 days by MTT assay Cytotoxicity against human HepG2 cells after 5 days by MTT assay	[PMID: 19615898]
HL-60	IC₅₀	12.2 μM Compound: NDGA	Cytotoxicity against human HL60 cells by XTT assay Cytotoxicity against human HL60 cells by XTT assay	[PMID: 16562834]
HL-60	IC₅₀	2.3 μM Compound: NDGA	Antioxidant activity in human HL60 cells assessed as inhibition of TPA-stimulated hydrogen peroxide induced DCFH-DA oxidation by fluorometric microplate assay Antioxidant activity in human HL60 cells assessed as inhibition of TPA-stimulated hydrogen peroxide induced DCFH-DA oxidation by fluorometric microplate assay	[PMID: 16562834]
HT-29	IC₅₀	51.3 μM Compound: NDGA	Cytotoxicity against human HT-29 cells after 5 days by MTT assay Cytotoxicity against human HT-29 cells after 5 days by MTT assay	[PMID: 19615898]
L929	EC₅₀	19 μM Compound: nordihydroguaiaretic acid	Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by [methyl-3H]thymidine incorporation assay Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by [methyl-3H]thymidine incorporation assay	[PMID: 9287415]
L929	EC₅₀	28 μM Compound: nordihydroguaiaretic acid	Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining	[PMID: 9287415]
LNCaP	IC₅₀	38.8 μM Compound: 4, ZINC00012342, Nordihydroguaiaretic acid	Transcriptional activity at human androgen receptor BF3 site stably transfected in eGFP-expressing human LNCAP cells after 5 days by fluorometric analysis Transcriptional activity at human androgen receptor BF3 site stably transfected in eGFP-expressing human LNCAP cells after 5 days by fluorometric analysis	[PMID: 22047606]
Macrophage	IC₅₀	6 μM Compound: NDGA	Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced LTC4 release by Ellman's method Antiinflammatory activity in NMRI mouse macrophages assessed as inhibition of A23187-induced LTC4 release by Ellman's method	[PMID: 8988605]
MCF7	IC₅₀	8.5 μM Compound: NDGA	Cytotoxicity against human MCF7 cells after 5 days by MTT assay Cytotoxicity against human MCF7 cells after 5 days by MTT assay	[PMID: 19615898]
MGC-803	IC₅₀	45.8 μM Compound: NDGA	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 27829519]
RBL-1	IC₅₀	0.12 μM Compound: NDGA	Inhibition of 5-lipoxygenase by measuring 5-HETE levels in RBL-1 cell-free supernatant Inhibition of 5-lipoxygenase by measuring 5-HETE levels in RBL-1 cell-free supernatant	[PMID: 8568814]
RBL-1	IC₅₀	0.15 μM Compound: NDGA (Nordihydroguaiaretic aid)	Ability to inhibit 5-lipoxygenase by using a crude preparation of the cytosolic enzyme from the rat basophilic leukemia (RBL-1) cell line Ability to inhibit 5-lipoxygenase by using a crude preparation of the cytosolic enzyme from the rat basophilic leukemia (RBL-1) cell line	[PMID: 2104936]
SGC-7901	IC₅₀	> 60 μM Compound: NDGA	Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay	[PMID: 27829519]

体外研究
(In Vitro)

天然的双酚 Nordihydroguaiaretic acid (NDGA) 是一种来自杂酚油植物 (Larrea tridentata：Zygophyllaceae) 的选择性 5LOX 抑制剂。抑制 5LOX 的天然双酚 Nordihydroguaiaretic acid 是一种非常有效、无毒的 TNFα 刺激的小胶质细胞激活拮抗剂。Nordihydroguaiaretic acid 在体外的效力大约是 Minocycline 的 6 倍，IC₅₀ 值为 8±3 μM，在 100 μM 时无毒性。在 800 nM Nordihydroguaiaretic acid 下观察到显著的 NO₂^- 抑制。对于天然和合成的 Nordihydroguaiaretic acid 以及 Nordihydroguaiaretic acid 的乙酰酯，观察到类似的功效。Nordihydroguaiaretic acid 还抑制 EOC-20 细胞受 TNFα 刺激的 PGE 生成₂，IC₅₀ 为 841 nM^[1]。前列腺素 E1 和 Nordihydroguaiaretic acid (NDGA) 对癌细胞系的增殖作用，HepG2 细胞系分别用不同剂量的两种化合物和阳性化合物 8-苯胺基-1-萘磺酸盐 (ANS) 处理 24 小时和通过 MTT 测定检查细胞活力。ANS 表现出剂量依赖性抑制作用 (0、10、30、50、80、100、120 和 150 μM)，估计的 IC₅₀ 为 25.888 μM。在 0、30、60、80、100、120、140 μM 不同浓度下，前列腺素 E1 和 Nordihydroguaiaretic acid 的检测 IC₅₀ 分别为 41.223 μM 和 45.646 μM^[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 ob/ob 饮食组相比，高剂量 Nordihydroguaiaretic acid (NDGA) 饮食组从 9 周开始体重显著下降，而从 12 周开始低剂量组。Nordihydroguaiaretic acid 处理导致 ob/ob 小鼠的体温 (直肠) 温度升高，尤其是在高剂量 Nordihydroguaiaretic acid^[3]时。

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

Clinical Trial

分子量

302.36

Formula

C₁₈H₂₂O₄

CAS 号

500-38-9

性状

固体

颜色

White to yellow

中文名称

去甲二氢愈创木酸；降二氫癒創木酸；正二氢愈创酸

结构分类

初始来源

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Store at room temperature 3 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 : 250 mg/mL (826.83 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	3.3073 mL	16.5366 mL	33.0732 mL
5 mM	0.6615 mL	3.3073 mL	6.6146 mL
10 mM	0.3307 mL	1.6537 mL	3.3073 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)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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: ≥ 2.08 mg/mL (6.88 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.88 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.88 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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

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: 99.93%

选择批次：

Data Sheet (659 KB) SDS (392 KB)

COA (283 KB) HNMR (263 KB) RP-HPLC (243 KB) LCMS (251 KB)

产品使用指南 (1538 KB)

参考文献

[1]. West M, et al. The arachidonic acid 5-lipoxygenase inhibitor Nordihydroguaiaretic acid inhibits tumor necrosis factor alpha activation of microglia and extends survival of G93A-SOD1 transgenic mice. J Neurochem. 2004 Oct;91(1):133-43. [Content Brief]

[2]. Lu F, et al. Virtual Screening for Potential Allosteric Inhibitors of Cyclin-Dependent Kinase 2 from Traditional Chinese Medicine. Molecules. 2016 Sep 21;21(9). pii: E1259. [Content Brief]

[3]. Zhang H, et al. Nordihydroguaiaretic acid improves metabolic dysregulation and aberrant hepatic lipid metabolism in mice by both PPARα-dependent and -independent pathways. Am J Physiol Gastrointest Liver Physiol. 2013 Jan 1;304(1):G72-86. [Content Brief]

Cell Assay ^[2]	MTT assay is used to measure cell growth-inhibitory activity of the selected most promising compounds in HepG2 cell lines. Cells are cultured in 96-well culture plate at 1×10⁴ cells/well. After 24 h cultured at 37 °C in the atmosphere of 5% CO₂, cells are adhered and treated with different concentrations of the targeted compounds (e.g., Nordihydroguaiaretic acid, 0, 30, 60, 80, 100, 120, and 140 μM) and incubated for 24 h. Then, the supernatants are discarded and MTT (0.5 mg/mL) is added to each well and incubated at 37°C in 5% CO₂ for an additional 4 h. Following, the MTT is removed and 150 μL of formazan in DMSO is added to terminate response and then plates are set to the table shaker for 5 min at low speed. Cell proliferation is evaluated by measuring the absorbance at 570 nm using ELISA Plate Reader. The IC₅₀ values are calculated by SPSS statistics 17.0^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] *Seven-week-old male control C57BL/6J mice, male leptin-deficient (ob/ob) mice, and male Pparα-deficient mutant mice (B6.129S4-Pparatm1Gonz/J)* are used. These mice are fed a standard chow diet for 1 wk to allow them to acclimatize to a controlled new environment (25±2°C, 55±5% relative humidity with a 12-h light-dark cycle). Subsequently, one group of ob/ob mice is switched to a chow diet supplemented with either low- (0.83 g/kg chow diet) or high-dose (2.5 g/kg chow diet) Nordihydroguaiaretic acid and maintained on this diet for 16 wk. The other groups of ob/ob mice and control mice continue to be fed a normal chow diet for 16 wk. In another set of studies, C57BL/6J mice and Pparα-deficient mutant mice are fed either a high-fat diet (~60% of total calories come from fat), or the same high-fat diet supplemented with a high dose of Nordihydroguaiaretic acid (2.5 g/kg diet). Food intake and body weights are measured once a week throughout the experiment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. West M, et al. The arachidonic acid 5-lipoxygenase inhibitor Nordihydroguaiaretic acid inhibits tumor necrosis factor alpha activation of microglia and extends survival of G93A-SOD1 transgenic mice. J Neurochem. 2004 Oct;91(1):133-43. [Content Brief] [2]. Lu F, et al. Virtual Screening for Potential Allosteric Inhibitors of Cyclin-Dependent Kinase 2 from Traditional Chinese Medicine. Molecules. 2016 Sep 21;21(9). pii: E1259. [Content Brief] [3]. Zhang H, et al. Nordihydroguaiaretic acid improves metabolic dysregulation and aberrant hepatic lipid metabolism in mice by both PPARα-dependent and -independent pathways. Am J Physiol Gastrointest Liver Physiol. 2013 Jan 1;304(1):G72-86. [Content Brief]

Nordihydroguaiaretic acid 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3073 mL	16.5366 mL	33.0732 mL	82.6829 mL
	5 mM	0.6615 mL	3.3073 mL	6.6146 mL	16.5366 mL
	10 mM	0.3307 mL	1.6537 mL	3.3073 mL	8.2683 mL
	15 mM	0.2205 mL	1.1024 mL	2.2049 mL	5.5122 mL
	20 mM	0.1654 mL	0.8268 mL	1.6537 mL	4.1341 mL
	25 mM	0.1323 mL	0.6615 mL	1.3229 mL	3.3073 mL
	30 mM	0.1102 mL	0.5512 mL	1.1024 mL	2.7561 mL
	40 mM	0.0827 mL	0.4134 mL	0.8268 mL	2.0671 mL
	50 mM	0.0661 mL	0.3307 mL	0.6615 mL	1.6537 mL
	60 mM	0.0551 mL	0.2756 mL	0.5512 mL	1.3780 mL
	80 mM	0.0413 mL	0.2067 mL	0.4134 mL	1.0335 mL
	100 mM	0.0331 mL	0.1654 mL	0.3307 mL	0.8268 mL

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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:

Nordihydroguaiaretic acid500-38-9NDGA去甲二氢愈创木酸降二氫癒創木酸正二氢愈创酸LipoxygenaseAutophagyFerroptosisLOXInhibitorinhibitorinhibit

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Nordihydroguaiaretic acid (Synonyms: 去甲二氢愈创木酸; NDGA)

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Other Forms of Nordihydroguaiaretic acid:

MCE 顾客使用本产品发表的 4 篇科研文献

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•相关化合物库:

•同靶点产品:

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实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Nordihydroguaiaretic acid 相关分类

完整储备液配制表

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Nordihydroguaiaretic acid (Synonyms: 去甲二氢愈创木酸; NDGA)

Customer Review

Other Forms of Nordihydroguaiaretic acid:

Nordihydroguaiaretic acid 相关抗体

MCE 顾客使用本产品发表的 4 篇科研文献

Nordihydroguaiaretic acid 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Lipoxygenase 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

Nordihydroguaiaretic acid 相关抗体:

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稀释计算器

Nordihydroguaiaretic acid 相关分类

完整储备液配制表

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