Lapachol (Synonyms: 拉帕醇)

目录号: HY-N6961 纯度: 99.06%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Lapachol 是一种天然萘醌，是一种具有口服活性的，有效的 DHODH 抑制剂。Lapachol 通过直接阻断 DHODH 活性的能力，从而抑制嘧啶合成，从而对淋巴细胞具有免疫抑制活性。Lapachol 是一种维生素 K 拮抗剂，具有抗肿瘤活性，可以抑制肿瘤细胞中 DNA 和 RNA 的合成。Lapachol 具有抗利什曼原虫活性。

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Lapachol Chemical Structure

CAS No. : 84-79-7

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规格	价格	是否有货
5 mg	￥312	In-stock
10 mg	￥500	In-stock
25 mg	￥725	In-stock
50 mg	￥1000	In-stock
100 mg	￥1500	In-stock
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500 mg		询价

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Customer Review

Other Forms of Lapachol:

Lapachol (Standard) 询价

MCE 顾客使用本产品发表的 2 篇科研文献

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
纯度 & 产品资料
参考文献

生物活性

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity^[1]^[2]^[3].

IC₅₀ & Target

Plasmodium

Leishmania

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	GI₅₀	1.9 μM Compound: 3	Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay	[PMID: 20304655]
A549	IC₅₀	> 30 μM Compound: 3	Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay	[PMID: 32044231]
A549	CC₅₀	≥ 285 μM Compound: 28	Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay	[PMID: 33333397]
A549	EC₅₀	4.78 μM Compound: 3	Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay	[PMID: 19674905]
A549	IC₅₀	8 μM Compound: 1, Lapachol	Growth inhibition of human A549 cells by MTT assay Growth inhibition of human A549 cells by MTT assay	[PMID: 24374273]
DU-145	IC₅₀	64.59 nM Compound: 1	Anticancer activity against human DU145 cells after 72 hrs by XTT assay Anticancer activity against human DU145 cells after 72 hrs by XTT assay	[PMID: 18829316]
ECa-109 cell line	IC₅₀	12.56 μM Compound: Lapachol	Cytotoxicity against human ECA109 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay Cytotoxicity against human ECA109 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay	[PMID: 27667553]
HBL-100	GI₅₀	7.8 μM Compound: 1	Growth inhibition of human HBL100 cells by SRB assay Growth inhibition of human HBL100 cells by SRB assay	[PMID: 22560628]
HBL-100	GI₅₀	7.8 μM Compound: 3	Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay	[PMID: 20304655]
HeLa	GI₅₀	2.3 μM Compound: 1	Growth inhibition of human HeLa cells by SRB assay Growth inhibition of human HeLa cells by SRB assay	[PMID: 22560628]
HeLa	GI₅₀	2.3 μM Compound: 3	Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay	[PMID: 20304655]
HeLa	IC₅₀	20.36 μM Compound: Lapachol	Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay	[PMID: 27667553]
HepG2	CC₅₀	> 4130.7 μM Compound: 1	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 29324340]
HepG2	CC₅₀	≥ 285 μM Compound: 28	Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay	[PMID: 33333397]
HL-60	IC₅₀	3.18 μM Compound: 1	Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay	[PMID: 17249647]
Hs 683	IC₅₀	11 μM Compound: 1, Lapachol	Growth inhibition of human Hs683 cells by MTT assay Growth inhibition of human Hs683 cells by MTT assay	[PMID: 24374273]
HT-29	EC₅₀	2.84 μM Compound: Lapachol	Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay	[PMID: 24900447]
HT-29	IC₅₀	4.66 μM Compound: Lapachol	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins	[PMID: 24900447]
K562	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay	[PMID: 30003778]
LLC-PK1	CC₅₀	≥ 285 μM Compound: 28	Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay	[PMID: 33333397]
LoVo	IC₅₀	9 μM Compound: 1, Lapachol	Growth inhibition of human LoVo cells by MTT assay Growth inhibition of human LoVo cells by MTT assay	[PMID: 24374273]
MCF7	IC₅₀	> 30 μM Compound: 3	Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay	[PMID: 32044231]
MCF7	EC₅₀	10.15 μM Compound: 3	Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay	[PMID: 19674905]
MDA-MB-231	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay	[PMID: 30003778]
MDA-MB-231	IC₅₀	> 30 μM Compound: 3	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay	[PMID: 32044231]
MRC5	CC₅₀	≥ 285 μM Compound: 28	Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay	[PMID: 33333397]
PBMC	IC₅₀	> 103.19 μM Compound: 1	Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay	[PMID: 21820768]
PBMC	IC₅₀	2.1 μM Compound: 1, Lapachol	Cytotoxicity against human PBMC after 72 hrs by alamar blue assay Cytotoxicity against human PBMC after 72 hrs by alamar blue assay	[PMID: 20378360]
PC-3	EC₅₀	1.97 μM Compound: 3	Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay	[PMID: 19674905]
PC-3	IC₅₀	4 μM Compound: 1, Lapachol	Growth inhibition of human PC3 cells by MTT assay Growth inhibition of human PC3 cells by MTT assay	[PMID: 24374273]
Peritoneal macrophage cell	CC₅₀	59.3 μM Compound: 10, Lapachol	Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay	[PMID: 23535320]
Raji	IC₅₀	311.4 μM Compound: 3	Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique	[PMID: 19674905]
SK-MEL-28	IC₅₀	8 μM Compound: 1, Lapachol	Growth inhibition of human SK-MEL-28 cells by MTT assay Growth inhibition of human SK-MEL-28 cells by MTT assay	[PMID: 24374273]
SW1573	GI₅₀	34 μM Compound: 1	Growth inhibition of human SW1573 cells by SRB assay Growth inhibition of human SW1573 cells by SRB assay	[PMID: 22560628]
SW1573	GI₅₀	34 μM Compound: 3	Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay	[PMID: 20304655]
T47D	GI₅₀	76 μM Compound: 3	Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay	[PMID: 20304655]
U2OS	EC₅₀	47.9 μM Compound: Lapachol	Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay	[PMID: 24900447]
U-373MG ATCC	IC₅₀	8 μM Compound: 1, Lapachol	Growth inhibition of human U373 cells by MTT assay Growth inhibition of human U373 cells by MTT assay	[PMID: 24374273]
WiDr	GI₅₀	36 μM Compound: 1	Growth inhibition of human WiDr cells by SRB assay Growth inhibition of human WiDr cells by SRB assay	[PMID: 22560628]
WiDr	GI₅₀	36 μM Compound: 3	Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay	[PMID: 20304655]

体外研究
(In Vitro)

Lapachol (10-100 μM；4 天) 通过抑制嘧啶生物合成来抑制淋巴细胞增殖^[1]。

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

Cell Proliferation Assay^[1]

Cell Line:	Murine CD4 T cells
Concentration:	10, 30, 100 μM
Incubation Time:	4 days
Result:	Inhibited the proliferation of murine CD4 T cells in a dose-dependent manner.

体内研究
(In Vivo)

Lapachol (3, 10 mg/kg；口服灌胃；每天一次，持续 4 周) 可降低 CIA 小鼠模型中实验性关节炎的严重程度^[1]。
Lapachol (10 mg/kg；口服灌胃；每天一次，持续 9 天) 在患有抗原诱导性关节炎 (AIA) 的雄性 C57BL/6 小鼠中，显示出膝关节白细胞浸润显着减少^[1]。

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

Animal Model:	Male DBA1/J mice (10-12 weeks old) with collagen-induced arthritis (CIA) models^[1]
Dosage:	3 mg/kg and 10 mg/kg
Administration:	Orally; once a day for 4 weeks
Result:	Markedly attenuated the severity of arthritis in CIA mice at both doses. Markedly reduced all histopathological features of arthritis severity.

分子量

242.27

Formula

C₁₅H₁₄O₃

CAS 号

84-79-7

性状

固体

颜色

Light yellow to yellow

中文名称

拉帕醇

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, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 66.67 mg/mL (275.19 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	4.1276 mL	20.6381 mL	41.2763 mL
5 mM	0.8255 mL	4.1276 mL	8.2553 mL
10 mM	0.4128 mL	2.0638 mL	4.1276 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 (stored under nitrogen)。-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)

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: ≥ 2.5 mg/mL (10.32 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。

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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.06%

选择批次：

Data Sheet (637 KB) SDS (393 KB)

COA (286 KB) HNMR (237 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Raphael S Peres, et al. Lapachol, a compound targeting pyrimidine metabolism, ameliorates experimental autoimmune arthritis. Arthritis Res Ther. 2017 Mar 7;19(1):47. [Content Brief]

[2]. Masayo Maeda, et al. Promotion or suppression of experimental metastasis of B16 melanoma cells after oral administration of lapachol. Toxicol Appl Pharmacol. 2008 Jun 1;229(2):232-8. [Content Brief]

[3]. Iasmin Aparecida Cunha Araújo, et al. Efficacy of lapachol on treatment of cutaneous and visceral leishmaniasis. Exp Parasitol. 2019 Apr:199:67-73. [Content Brief]

Lapachol 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	4.1276 mL	20.6381 mL	41.2763 mL	103.1907 mL
	5 mM	0.8255 mL	4.1276 mL	8.2553 mL	20.6381 mL
	10 mM	0.4128 mL	2.0638 mL	4.1276 mL	10.3191 mL
	15 mM	0.2752 mL	1.3759 mL	2.7518 mL	6.8794 mL
	20 mM	0.2064 mL	1.0319 mL	2.0638 mL	5.1595 mL
	25 mM	0.1651 mL	0.8255 mL	1.6511 mL	4.1276 mL
	30 mM	0.1376 mL	0.6879 mL	1.3759 mL	3.4397 mL
	40 mM	0.1032 mL	0.5160 mL	1.0319 mL	2.5798 mL
	50 mM	0.0826 mL	0.4128 mL	0.8255 mL	2.0638 mL
	60 mM	0.0688 mL	0.3440 mL	0.6879 mL	1.7198 mL
	80 mM	0.0516 mL	0.2580 mL	0.5160 mL	1.2899 mL
	100 mM	0.0413 mL	0.2064 mL	0.4128 mL	1.0319 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:

Lapachol84-79-7拉帕醇Dihydroorotate DehydrogenaseDNA/RNA SynthesisParasiteDHODHnaphthoquinoneimmunosuppressivelymphocytespyrimidine synthesisvitamin Kantitumorneoplastic cellsanti-LeishmaniaInhibitorinhibitorinhibit

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Lapachol (Synonyms: 拉帕醇)

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MCE 顾客使用本产品发表的 2 篇科研文献

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参考文献

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稀释计算器

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完整储备液配制表

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Lapachol (Synonyms: 拉帕醇)

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Lapachol 相关抗体

MCE 顾客使用本产品发表的 2 篇科研文献

Lapachol 相关产品

•相关化合物库:

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查看 Parasite 亚型特异性产品:

生物活性

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参考文献

Lapachol 相关抗体:

摩尔计算器

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Lapachol 相关分类

完整储备液配制表

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