L-165041
Based on 2 publication(s) in Google Scholar
L-165041 is a cell permeable PPARδ agonist, with Kis 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.
- Purity: 99.12%
- CAS No.: 79558-09-1
- Formula: C22H26O7
- Molecular Weight:402.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) L-165041
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Biological Activity
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PPARδ 6 nM (Ki) |
PPARγ 730 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-1 | EC50 |
0.021 μM
Compound: L-165041
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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
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[PMID: 22081932] |
| COS-7 | EC50 |
0.039 μM
Compound: L-165041
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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
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[PMID: 23130964] |
| COS-7 | EC50 |
0.039 μM
Compound: L-165041
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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
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[PMID: 26595749] |
| COS-7 | EC50 |
125 nM
Compound: L-165041
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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
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[PMID: 16797985] |
| COS-7 | EC50 |
1824 nM
Compound: L-165041
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Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells
Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells
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[PMID: 16797985] |
| COS-7 | EC50 |
977 nM
Compound: L-165041
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Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells
Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells
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[PMID: 16797985] |
| HEK293 | EC50 |
0.021 μM
Compound: L-165,041
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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
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10.1039/C5MD00151J |
| HepG2 | EC50 |
0.021 μM
Compound: L-165,041
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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
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[PMID: 25462281] |
| HepG2 | EC50 |
0.21 μM
Compound: L165,041
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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
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[PMID: 30996794] |
| HepG2 | EC50 |
0.64 μM
Compound: L-165041
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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
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[PMID: 22381047] |
| HepG2 | EC50 |
0.65 μM
Compound: L-165041
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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
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[PMID: 23031596] |
L-165041 is a PPARδ agonist, with Kis 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 79558-09-1
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Appearance Solid
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Molecular Weight 402.44
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Formula C22H26O7
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Color White to off-white
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SMILES
O=C(O)COC(C=C1)=CC=C1OCCCOC2=CC=C(C(C)=O)C(O)=C2CCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Bioorg Chem
Discovery of Tetrazolone derivatives as potent PPARα/δ dual agonists for metabolic dysfunction-associated steatohepatitis. [Abstract]2026 Jul 5:175:109764. PMID: 41880786 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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]
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.
| 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 |
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