L-165041

Name: L-165041
Brand: MedChemExpress
SKU: HY-20019
Rating: 4.5 (1 reviews)

Cat. No.: HY-20019 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

L-165041 Chemical Structure

CAS No. : 79558-09-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

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]

In Vitro

L-165041 is a PPARδ agonist, with K_is of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively^[1]. L-165041 (1 or 5 μM) inhibits VEGF-induced endothelial cells (ECs) proliferation and migration. L-165041 negatively affects cell cycle progression in VEGF-activated human umbilical vein ECs (HUVECs). L-165041 (10 μM)inhibits PPARδ-independent, VEGF-induced angiogenesis^[2]. PPARδ ligand L-165041 inhibits PDGF-induced rVSMC proliferation and migration. With 1 h of L-165041 pretreatment, PDGF-induced cellular migration is inhibited. L-165041 (10 μM) significantly suppresses S phase transition induced by PDGF^[4].

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

In Vivo

L-165041 (5 mg/kg/day, i.p.) significantly lowers the formation of lipid droplets in mice. L-165041 markedly reduces the level of both the hepatic cholesterol and triglycerides in mice. L-165041 increases mRNA expression levels of PPARδ compared to the vehicle group. Lipoprotein lipase (LPL) expression in L-165041-treated mice is significantly higher than that in the vehicle group^[3].

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

Molecular Weight

402.44

Formula

C₂₂H₂₆O₇

CAS No.

79558-09-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)COC(C=C1)=CC=C1OCCCOC2=CC=C(C(C)=O)C(O)=C2CCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (124.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (244 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

L-165041 Related Classifications

Metabolic Disease

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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L-165041

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Complete Stock Solution Preparation Table

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