Licofelone (Synonyms: ML-3000)

目录号: HY-B1452 纯度: 98.62%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Licofelone (ML-3000) 是双 COX/5-LOX 抑制剂 (IC₅₀ 分别为 0.21，0.18 μM)，有潜力用于骨关节炎的研究。Licofelone 具有抗炎和抗增殖作用。Licofelone 诱导细胞凋亡，减少促炎性白三烯和前列腺素的产生。

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Licofelone Chemical Structure

CAS No. : 156897-06-2

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规格	价格	是否有货
1 mg	￥300	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
25 mg	￥1600	In-stock
50 mg	￥2400	In-stock
100 mg	￥3713	In-stock
200 mg	￥5350	In-stock
500 mg		询价
1 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Licofelone:

Licofelone-d4 询价
Licofelone-d₆ 询价

MCE 顾客使用本产品发表的 1 篇科研文献

•Clin Nutr. 2023 Dec 30;43(2):453-467. [Abstract]

Licofelone 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 COX 亚型特异性产品:

查看所有亚型

COX COX-1 COX-2 COX-3

查看 Lipoxygenase 亚型特异性产品:

查看所有亚型

5-LOX 12-LOX 15-LOX

生物活性
纯度 & 产品资料
参考文献

生物活性

Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC₅₀=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins^[1]^[2]^[3].

IC₅₀ & Target^[3]

COX

0.21 μM (IC₅₀)

5-LOX

0.18 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	6 μM Compound: 3, ML3000	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as blockade of PGH2 to PGE2 conversion after 1 min Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as blockade of PGH2 to PGE2 conversion after 1 min	[PMID: 19719242]
A549	IC₅₀	6.7 μM Compound: 3, ML3000	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method	[PMID: 19719242]
HeLa	IC₅₀	6 μM Compound: Licofelone	Inhibition of mPGES1 in human HeLa cells assessed as reduction in TNF-alpha induced PGE2 production preincubated for 2 hrs followed by TNF-alpha addition for 24 hrs by ELISA Inhibition of mPGES1 in human HeLa cells assessed as reduction in TNF-alpha induced PGE2 production preincubated for 2 hrs followed by TNF-alpha addition for 24 hrs by ELISA	[PMID: 27597418]
HT-29	IC₅₀	21.1 μM Compound: Licofelone	Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24295787]
HT-29	IC₅₀	67 μM Compound: Licofelone	Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay	[PMID: 24295787]
MCF7	IC₅₀	36.7 μM Compound: Licofelone	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs	[PMID: 21295381]
MDA-MB-231	IC₅₀	5.5 μM Compound: Licofelone	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs	[PMID: 21295381]
SW480	IC₅₀	68 μM Compound: Licofelone	Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay	[PMID: 24295787]

体外研究
(In Vitro)

Licofelone 对人血小板 COX 和人 5-LO 的 IC₅₀ 分别为 0.16 μM 和 0.23 μM^[3]。

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

分子量

379.88

Formula

C₂₃H₂₂ClNO₂

CAS 号

156897-06-2

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (65.81 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	2.6324 mL	13.1621 mL	26.3241 mL
5 mM	0.5265 mL	2.6324 mL	5.2648 mL
10 mM	0.2632 mL	1.3162 mL	2.6324 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。-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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.58 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，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 25.0 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: ≥99.0%

选择批次：

Data Sheet (623 KB) SDS (393 KB)

COA (177 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Tavolari S, et al. Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis. 2008 Feb;29(2):371-80. [Content Brief]

[2]. Alvaro-Gracia JM, et al. Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis. Rheumatology (Oxford). 2004 Feb;43 Suppl 1:i21-5. [Content Brief]

[3]. Laufer SA, et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J Med Chem. 1994 Jun 10;37(12):1894-7. [Content Brief]

Licofelone 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	2.6324 mL	13.1621 mL	26.3241 mL	65.8103 mL
	5 mM	0.5265 mL	2.6324 mL	5.2648 mL	13.1621 mL
	10 mM	0.2632 mL	1.3162 mL	2.6324 mL	6.5810 mL
	15 mM	0.1755 mL	0.8775 mL	1.7549 mL	4.3874 mL
	20 mM	0.1316 mL	0.6581 mL	1.3162 mL	3.2905 mL
	25 mM	0.1053 mL	0.5265 mL	1.0530 mL	2.6324 mL
	30 mM	0.0877 mL	0.4387 mL	0.8775 mL	2.1937 mL
	40 mM	0.0658 mL	0.3291 mL	0.6581 mL	1.6453 mL
	50 mM	0.0526 mL	0.2632 mL	0.5265 mL	1.3162 mL
	60 mM	0.0439 mL	0.2194 mL	0.4387 mL	1.0968 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:

Licofelone156897-06-2ML-3000ML3000ML 3000COXLipoxygenaseApoptosisCyclooxygenaseLOXInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Licofelone (Synonyms: ML-3000)

Customer Review

Other Forms of Licofelone:

MCE 顾客使用本产品发表的 1 篇科研文献