GW501516 (Synonyms: GW 1516) |
Catalog No.GC15318
One-Click Copy Product Info
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GW501516 is a synthetic PPARδ-specific agonist, with an EC50 of 0.10nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 317318-70-0
Sample solution is provided at 25 µL, 10mM.
GW501516 is a synthetic PPARδ-specific agonist, with an EC50 of 0.10nM [1]. Activation of PPARβ/δ by GW501516 in skeletal muscle cells induces the expression of genes involved in preferential lipid utilization, β-oxidation, cholesterol efflux, and energy uncoupling[2]. GW501516 can regulate the plasma lipid metabolism in animals and has been widely used as a model compound for the development of a series of new derivatives[3].
In vitro, GW501516 treatment at a concentration of 2500nM for 72 hours significantly inhibited cell proliferation and colony formation of C666-1 cells, resulting in impaired cell cycle progression[4]. The pretreatment of human pulmonary artery smooth muscle cells with GW501516 (3000nM) for 6 hours could significantly inhibit the cell migration and collagen synthesis induced by Platelet-derived growth factor (PDGF) (10ng/mL; 24 hours) [5]. GW501516 treatment (100nM) for 24 hours induced the release of growth factor in human vascular endothelial cells, as well as the expression of adipocyte differentiation-related protein (ADRP), stimulating cell proliferation and morphogenesis[6].
In vivo, GW501516 treatment (10μg/kg/day; p.o.) for 6 weeks increased liver fibrosis induced by CCl4 in mice, and increased the expression of pro-inflammatory markers and the infiltration of macrophages in the liver[7]. Intraperitoneal injection of GW501516 (2mg/kg) 6 hours before lipopolysaccharide (LPS) administration can reduce the mortality rate and liver damage in mice with acute liver failure, and lower the levels of pro-inflammatory cytokines in the serum[8].
References:
[1] Wei Z L, Kozikowski A P. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor δ[J]. The Journal of organic chemistry, 2003, 68(23): 9116-9118.
[2] Dressel U, Allen T L, Pippal J B, et al. The peroxisome proliferator-activated receptor β/δ agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells[J]. Molecular endocrinology, 2003, 17(12): 2477-2493.
[3] Ciocoiu C C, Ravna A W, Sylte I, et al. Synthesis, biological evaluation and molecular modeling of GW 501516 analogues[J]. Archiv der Pharmazie, 2010, 343(11‐12): 612-624.
[4] Ji Y, Li H, Wang F, et al. PPARβ/δ agonist GW501516 inhibits tumorigenicity of undifferentiated nasopharyngeal carcinoma in C666-1 cells by promoting apoptosis[J]. Frontiers in pharmacology, 2018, 9: 648.
[5] Liu G, Li X, Li Y, et al. PPARδ agonist GW501516 inhibits PDGF‐stimulated pulmonary arterial smooth muscle cell function related to pathological vascular remodeling[J]. BioMed research international, 2013, 2013(1): 903947.
[6] Piqueras L, Reynolds A R, Hodivala-Dilke K M, et al. Activation of PPARβ/δ induces endothelial cell proliferation and angiogenesis[J]. Arteriosclerosis, thrombosis, and vascular biology, 2007, 27(1): 63-69.
[7] Kostadinova R, Montagner A, Gouranton E, et al. GW501516-activated PPARβ/δ promotes liver fibrosis via p38-JNK MAPK-induced hepatic stellate cell proliferation[J]. Cell & bioscience, 2012, 2(1): 34.
[8] Lim H J, Kwak H J. Selective PPARδ Agonist GW501516 Protects Against LPS-Induced Macrophage Inflammation and Acute Liver Failure in Mice via Suppressing Inflammatory Mediators[J]. Molecules, 2024, 29(21): 5189.
| Cell experiment [1]: | |
Cell lines | Human umbilical vein endothelial cells |
Preparation Method | Human umbilical vein endothelial cells (HUVECs) were cultured in DMEM supplemented with 10% fetal bovine serum (FBS), antibiotic/antimycotic mix, and 1% hypoxanthine, aminopterin, and thymidine. HUVECs were seeded on extracellular matrix at 2×105 cells/well in 24-well plates in the absence of serum and incubated for 24 hours in the presence or absence of GW501516 (100nM). Phase contrast micrographs were recorded, and the mean number of tubes in 5 low-power (×100) random fields assessed. |
Reaction Conditions | 100nM; 24h |
Applications | GW501516 treatment significantly induces endothelial cell proliferation and enhance the number of HUVECs. |
| Animal experiment [2]: | |
Animal models | C57BL6/J mice |
Preparation Method | Male C57BL6/J (8 to 9 weeks old) mice, 20 to 25g, were kept in a specific pathogen-free environment at an animal-breeding facility. Mice were injected with lipopolysaccharide (LPS)/galactosamine (GalN) (20mg/700mg/kg) in saline as a single i.p. dose to induce acute liver failure. To investigate if GW501516 has an anti-inflammatory effect, mice were randomized into groups and treated with vehicle (0.1% DMSO; n = 8), LPS/GalN (n = 8) or LPS/GalN plus GW501516 (2mg/kg; n = 15). Intraperitoneal injection of GW501516 was done 6h before LPS administration. Five hours later, blood samples were collected by orbital puncture, and serum was prepared by centrifugation (12,000g for 20min at 4 °C) for IL-1β, IL-6, TNF-α, ALT, and AST levels measurement. |
Dosage form | 2mg/kg for a single dosage; i.p. |
Applications | GW501516 treatment significantly reduced the levels of pro-inflammatory cytokines in the mouse serum and increased the survival rate of the mice. |
References: | |
| Cas No. | 317318-70-0 | SDF | |
| Synonyms | GW 1516 | ||
| Chemical Name | 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid | ||
| Canonical SMILES | CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)OCC(=O)O | ||
| Formula | C21H18F3NO3S2 | M.Wt | 453.5 |
| Solubility | ≥ 18.05 mg/mL in DMSO, ≥ 44.6 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2051 mL | 11.0254 mL | 22.0507 mL |
| 5 mM | 441 μL | 2.2051 mL | 4.4101 mL |
| 10 mM | 220.5 μL | 1.1025 mL | 2.2051 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)