Lapachol (Synonyms: 拉帕醇)

目錄號: HY-N6961 純度: 99.06%: FAQs
Data Sheet SDS COA 產品使用指南技術支持

Lapachol 是一種天然萘醌，是一種具有口服活性的，有效的 DHODH 抑制劑。Lapachol 通過直接阻斷 DHODH 活性的能力，從而抑制嘧啶合成，從而對淋巴細胞具有免疫抑制活性。Lapachol 是一種維生素 K 拮抗劑，具有抗腫瘤活性，可以抑制腫瘤細胞中 DNA 和 RNA 的合成。Lapachol 具有抗利什曼原蟲活性。

MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務

Lapachol Chemical Structure

CAS No. : 84-79-7

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規(guī)格	價格	是否有貨
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
200 mg		詢價
500 mg		詢價

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Customer Review

Other Forms of Lapachol:

Lapachol (Standard) 詢價

Lapachol 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 Parasite 亞型特異性產品:

查看所有亞型

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
純度 & 產品資料
參考文獻

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

細胞效力
(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]

體外研究
(In Vitro)

Lapachol (10-100 μM；4 天) 通過抑制嘧啶生物合成來抑制淋巴細胞增殖^[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.

體內研究
(In Vivo)

Lapachol (3, 10 mg/kg；口服灌胃；每天一次，持續(xù) 4 周) 可降低 CIA 小鼠模型中實驗性關節(jié)炎的嚴重程度^[1]。
Lapachol (10 mg/kg；口服灌胃；每天一次，持續(xù) 9 天) 在患有抗原誘導性關節(jié)炎 (AIA) 的雄性 C57BL/6 小鼠中，顯示出膝關節(jié)白細胞浸潤顯著減少^[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 號

84-79-7

性狀

固體

顏色

Light yellow to yellow

中文名稱

拉帕醇

結構分類

初始來源

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, stored under nitrogen

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

溶解性數據

細胞實驗：

DMSO 中的溶解度 : 66.67 mg/mL (275.19 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質量	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

查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

摩爾計算器
稀釋計算器

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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據您的實驗動物和給藥方式選擇適當的溶解方案。

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.32 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網站選購。，Tween 80，均可在 MCE 網站選購。

計算結果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

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

您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。

動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產品資料

純度: 99.06%

選擇批次：

Data Sheet (637 KB) SDS (393 KB)

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

產品使用指南 (1538 KB)

參考文獻

[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 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	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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生物活性

純度 & 產品資料

參考文獻

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稀釋計算器

Lapachol 相關分類

完整儲備液配制表

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Lapachol (Synonyms: 拉帕醇)

Customer Review

Other Forms of Lapachol:

Lapachol 相關抗體

MCE 顧客使用本產品發(fā)表的 2 篇科研文獻

Lapachol 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 Parasite 亞型特異性產品:

生物活性

純度 & 產品資料

參考文獻

Lapachol 相關抗體:

摩爾計算器

稀釋計算器

Lapachol 相關分類

完整儲備液配制表

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