L-165041

目录号: HY-20019 纯度: 99.67%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

L-165041 是一种细胞渗透的 PPARδ 激动剂，对 PPARδ 和 PPARγ 的 K_i 值分别为 6 nM 和约 730 nM，可以在 NIH-PPARδ 细胞中诱导脂肪细胞分化。

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L-165041 Chemical Structure

CAS No. : 79558-09-1

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规格	价格	是否有货
Free Sample (0.1 - 0.2 mg)		Apply now
10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥500	In-stock
10 mg	￥884	In-stock
50 mg	￥2700	In-stock
100 mg	￥4300	In-stock
200 mg		询价
500 mg		询价

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PPARα PPARβ/δ PPARγ PPAR PPARδ

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

L-165041 is a cell permeable PPARδ agonist, with K_is of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.

IC₅₀ & Target^[1]

PPARδ

6 nM (Ki)

PPARγ

730 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
COS-1	EC₅₀	0.021 μM Compound: L-165041	Agonist activity at human GAL4-fused PPARdelta ligand binding domain expressed in COS-1 cells after 20 hrs by luciferase reporter gene transactivation assay Agonist activity at human GAL4-fused PPARdelta ligand binding domain expressed in COS-1 cells after 20 hrs by luciferase reporter gene transactivation assay	[PMID: 22081932]
COS-7	EC₅₀	0.039 μM Compound: L-165041	Transactivation of human PPARdelta expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay Transactivation of human PPARdelta expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay	[PMID: 26595749]
COS-7	EC₅₀	0.039 μM Compound: L-165041	Transactivation of GAL4-fused human PPARdelta ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay Transactivation of GAL4-fused human PPARdelta ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay	[PMID: 23130964]
COS-7	EC₅₀	125 nM Compound: L-165041	Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells	[PMID: 16797985]
COS-7	EC₅₀	1824 nM Compound: L-165041	Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells	[PMID: 16797985]
COS-7	EC₅₀	977 nM Compound: L-165041	Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells	[PMID: 16797985]
HEK293	EC₅₀	0.021 μM Compound: L-165,041	Transactivation of human PPARdelta expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay Transactivation of human PPARdelta expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay	10.1039/C5MD00151J
HepG2	EC₅₀	0.021 μM Compound: L-165,041	Agonist activity at human GAL4-PPARdelta ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay Agonist activity at human GAL4-PPARdelta ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay	[PMID: 25462281]
HepG2	EC₅₀	0.21 μM Compound: L165,041	Transactivation of GAL4-tagged human PPARdelta LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay Transactivation of GAL4-tagged human PPARdelta LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay	[PMID: 30996794]
HepG2	EC₅₀	0.64 μM Compound: L-165041	Transactivation of GAL4-fused PPARbeta LBD expressed in HepG2 cells after 20 hrs by luminescence assay Transactivation of GAL4-fused PPARbeta LBD expressed in HepG2 cells after 20 hrs by luminescence assay	[PMID: 22381047]
HepG2	EC₅₀	0.65 μM Compound: L-165041	Transactivation of GAL4-fused PPARbeta (delta) ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay Transactivation of GAL4-fused PPARbeta (delta) ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay	[PMID: 23031596]

体外研究
(In Vitro)

L-165041 是一种 PPARδ 激动剂，对 PPARδ 和 PPARγ 的 K_i 分别为 6 nM 和大约 730 nM^[1]。
L-165041 (1 或 5 μM) 抑制 VEGF 诱导的内皮细胞 (EC) 增殖和迁移。L-165041 对 VEGF 激活的人脐静脉内皮细胞 (HUVEC) 的细胞周期进程产生负面影响。L-165041 (10 μM) 抑制 PPARδ 非依赖性、VEGF 诱导的血管生成^[2]。
PPARδ 配体 L-165041 抑制 PDGF 诱导的 rVSMC 增殖和迁移。L-165041 预处理 1 小时后，PDGF 诱导的细胞迁移受到抑制。L-165041 (10 μM) 显著抑制由 PDGF 诱导的 S 相转变^[4]。

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

体内研究
(In Vivo)

L-165041 (5 mg/kg/天，腹腔注射) 显著降低小鼠脂滴的形成。L-165041 显著降低小鼠肝脏胆固醇和甘油三酯的水平。与载体组相比，L-165041 增加了 PPARδ 的 mRNA 表达水平。L-165041 处理小鼠的脂蛋白脂肪酶 (LPL) 表达显著高于载体组^[3]。

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

分子量

402.44

Formula

C₂₂H₂₆O₇

CAS 号

79558-09-1

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 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 : 50 mg/mL (124.24 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	2.4848 mL	12.4242 mL	24.8484 mL
5 mM	0.4970 mL	2.4848 mL	4.9697 mL
10 mM	0.2485 mL	1.2424 mL	2.4848 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: ≥ 2.5 mg/mL (6.21 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。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.21 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: 99.67%

选择批次：

Data Sheet (638 KB) SDS (252 KB)

COA (281 KB) LCMS (268 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Berger J, et al. Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem. 1999 Mar 5;274(10):6718-25. [Content Brief]

[2]. Park, Jin-Hee., et al. The PPARδ ligand L-165041 inhibits vegf-induced angiogenesis, but the antiangiogenic effect is not related to PPARδ. Journal of Cellular Biochemistry (2012), 113(6), 1947-1954. [Content Brief]

[3]. Lim, Hyun-Joung., et al. PPARδ ligand L-165041 ameliorates Western diet-induced hepatic lipid accumulation and inflammation in LDLR-/- mice. European Journal of Pharmacology (2009), 622(1-3), 45-51. [Content Brief]

[4]. Lim, Hyun-Joung., et al. PPARδ agonist L-165041 inhibits rat vascular smooth muscle cell proliferation and migration via inhibition of cell cycle. Atherosclerosis (Amsterdam, Netherlands) (2009), 202(2), 446-454. [Content Brief]

Cell Assay ^[2]	Human umbilical vein ECs (HUVECs) are cultured in EGM-2. Subconfluent HUVECs are made quiescent by serum starvation [EBM-2 containing 0.1% fetal bovine serum (FBS)] for 4 h. The cells are pretreated with the PPARδ ligand L-165041 or GW501516 for 6 h followed by VEGF (10 ng/mL) induction ^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	LDLR^−/− mice are divided into vehicle (0.1 N NaOH) and L-165041 (5 mg/kg/day) group (9 animals in each group). LDLR^−/− mice receive either NaOH or L-165041 via daily intraperitoneal injection (i.p.) for 16 weeks with the Western diet. Body weight is measured once a week and the blood samples for a serum parameter analysis are collected using an eye-bleeding method every 4 weeks. At the end of the experiment, LDLR^−/− mice are fasted for 24 h before sacrificed and the liver samples are either fixed in formalin or frozen at −70°C for further analysis. All animals are housed in polycarbonate cages in a room with a 12-h light/12-h dark cycle, and maintained at a constant temperature of 22°C^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Berger J, et al. Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. J Biol Chem. 1999 Mar 5;274(10):6718-25. [Content Brief] [2]. Park, Jin-Hee., et al. The PPARδ ligand L-165041 inhibits vegf-induced angiogenesis, but the antiangiogenic effect is not related to PPARδ. Journal of Cellular Biochemistry (2012), 113(6), 1947-1954. [Content Brief] [3]. Lim, Hyun-Joung., et al. PPARδ ligand L-165041 ameliorates Western diet-induced hepatic lipid accumulation and inflammation in LDLR-/- mice. European Journal of Pharmacology (2009), 622(1-3), 45-51. [Content Brief] [4]. Lim, Hyun-Joung., et al. PPARδ agonist L-165041 inhibits rat vascular smooth muscle cell proliferation and migration via inhibition of cell cycle. Atherosclerosis (Amsterdam, Netherlands) (2009), 202(2), 446-454. [Content Brief]

L-165041 相关分类

Metabolic Disease

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	2.4848 mL	12.4242 mL	24.8484 mL	62.1211 mL
	5 mM	0.4970 mL	2.4848 mL	4.9697 mL	12.4242 mL
	10 mM	0.2485 mL	1.2424 mL	2.4848 mL	6.2121 mL
	15 mM	0.1657 mL	0.8283 mL	1.6566 mL	4.1414 mL
	20 mM	0.1242 mL	0.6212 mL	1.2424 mL	3.1061 mL
	25 mM	0.0994 mL	0.4970 mL	0.9939 mL	2.4848 mL
	30 mM	0.0828 mL	0.4141 mL	0.8283 mL	2.0707 mL
	40 mM	0.0621 mL	0.3106 mL	0.6212 mL	1.5530 mL
	50 mM	0.0497 mL	0.2485 mL	0.4970 mL	1.2424 mL
	60 mM	0.0414 mL	0.2071 mL	0.4141 mL	1.0354 mL
	80 mM	0.0311 mL	0.1553 mL	0.3106 mL	0.7765 mL
	100 mM	0.0248 mL	0.1242 mL	0.2485 mL	0.6212 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:

L-16504179558-09-1L165041L 165041PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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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）

L-165041