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  1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Anti-infection
  2. Dihydroorotate Dehydrogenase DNA/RNA Synthesis Parasite
  3. Lapachol

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(duì)淋巴細(xì)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(xì)胞中 DNA 和 RNA 的合成。Lapachol 具有抗利什曼原蟲活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Lapachol Chemical Structure

Lapachol Chemical Structure

CAS No. : 84-79-7

1.  客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2.  同一機(jī)構(gòu)(單位)同一產(chǎn)品試用裝僅限申領(lǐng)一次,同一機(jī)構(gòu)(單位)一年內(nèi)

     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

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5 mg ¥312
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10 mg ¥500
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25 mg ¥725
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100 mg ¥1500
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Customer Review

Other Forms of Lapachol:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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(xì)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(xì)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(nèi)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(shí)驗(yàn)性關(guān)節(jié)炎的嚴(yán)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(dǎo)性關(guān)節(jié)炎 (AIA) 的雄性 C57BL/6 小鼠中,顯示出膝關(guān)節(jié)白細(xì)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(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

拉帕醇

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 66.67 mg/mL (275.19 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)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。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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(chǎn)品資料

純度: 99.06%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱:
Lapachol
目錄號(hào):
HY-N6961
需求量: