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Purity: ≥98%
GW 501516 (also known as endurobol; GW-501516; GSK-516) is a novel and potent PPARδ agonist with an EC50 of 1.1 nM. Endurobol was withdrawn from clinical development in 2007 due to evidence from animal experiments that the medication caused cancer to spread quickly throughout multiple organs. Endurobol was initially being studied as a potential treatment for metabolic and cardiovascular disorders. When GW501516, a particular PPARβ/δ selective agonist, activated the PPARβ/δ ligand, it significantly reduced colony formation and cell proliferation in EBV positive undifferentiated NPC C666-1 cells, inducing a G2/M phase arrest in comparison to control cells. Furthermore, GW501516 induced apoptosis in C666-1 cells in a way that required both BAX and caspase. GW501516 significantly reduced the ectopic NPC xenograft tumorigenicity in BALB/c nu/nu mice, which was derived from the C666-1 NPC cells, in line with the in vitro result. Its suppression of integrin-linked kinase (ILK) gene and protein expression via AMPKα-dependent signaling pathways is closely linked to this effect. All together, we demonstrated that the degree of differentiation in NPC cell lines is inversely correlated with PPARβ/δ expression, and we demonstrated how GW501516 inhibits tumor growth in NPC cells by activating AMPKα. According to this study, PPARβ/δ targeting molecules may be helpful for chemoprevention of poorly differentiated NPCs in particular.
| Targets |
PPARδ (EC50 = 1.1 nM)
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| Cell Assay |
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| Animal Protocol |
Rats: At 12 weeks of age, female Sprague Dawley rats are divided into three groups: a control group (OVX-CTR), a low-dose GW 501516 (OVX-GW1), and a high-dose GW 501516 (OVX-GW5). For four months, the animals are gavaged with either GW 501516 or the vehicle (methylcellulose) every day. Dual x-ray absorptiometry is used to evaluate bone mineral density (BMD) at the femur, spine, and entire body[2].
Mice: Mice are given therapeutic diets and treatments, and they are divided into groups at random. To create the rodent diet containing GW 501516, GW 501516 is gradually added to the control diet until it reaches a final concentration of 0.04% w/w. 10% of the calories in the control diet are derived from fat (5.5% from soybean oil and 4.5% from lard)[3]. |
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| References |
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| Molecular Formula |
C21H18F3NO3S2
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| Molecular Weight |
453.497733592987
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| Exact Mass |
453.07
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| Elemental Analysis |
C, 55.62; H, 4.00; F, 12.57; N, 3.09; O, 10.58; S, 14.14
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| CAS # |
317318-70-0
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| Related CAS # |
317318-70-0
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)OCC(=O)O
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| InChi Key |
YDBLKRPLXZNVNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27)
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| Chemical Name |
2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid
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| Synonyms |
Endurobol; GSK516; GW1516; GW501516; GW 1516; GSK 516; GW-501516; GW-1516; GSK-516; GW 501516
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~51 mg/mL (~197.5 mM)
Water: ~20 mg/mL (~77.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.51 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+40% PEG 300+2% Tween 80+ddH2O: 6mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2051 mL | 11.0254 mL | 22.0507 mL | |
| 5 mM | 0.4410 mL | 2.2051 mL | 4.4101 mL | |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2051 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00158899 | Completed | Drug: GW501516 oral tablets | Dyslipidaemias Dyslipidaemia |
GlaxoSmithKline | August 2004 | Phase 2 |
| NCT00388180 | Completed | Drug: GW501516 Drug: GW590735 |
Dyslipidaemias Obesity |
GlaxoSmithKline | December 2004 | |
| NCT00841217 | Completed | Drug: GW501516 Drug: placebo pill |
Obesity Lipid Disorders |
The University of Western Australia |
April 2003 | Phase 4 |
| NCT00318617 | Terminated | Drug: GW510516X | Dyslipidaemias Heart Failure |
GlaxoSmithKline | December 2005 |
 The impact of GW501516 on cell proliferation and colony formation.
GW501516 inhibited gene and protein expression of integrin-linked kinase (ILK) in C666-1 cells.Front Pharmacol.2018 Jun 28;9:648. |
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 The impact of GW501516 on cell cycle of C666-1 cells.
GW501516 suppressed SS tumor growthin vivo.Front Pharmacol.2018 Jun 28;9:648. |
 The impact of GW501516 on apoptosis in C666-1 cells.
The impact of GW501516 on protein expression in C666-1 cells. The gene and protein expression of PPARβ/δ in nasopharyngeal carcinoma (NPC) cell lines.Front |
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