Calculated reference model · not an experimental or batch-certified structure. All 30 atoms shown.
Model data & sources
- Heavy atoms only; hydrogens are omitted from the reference display.
- Source-defined stereochemistry is checked against the calculated coordinates; no energy-minimum, crystal or solution-structure claim is made.
- Reference molecular species only; batch identity, purity, counterions and excipients are not certified.
- Formula
- C21H18F3NO3S2
- Method
- RDKit ETKDGv3 / MMFF94s calculated reference conformer
GW-501516
GW-501516 Research Standard
GW-501516 (CAS 317318-70-0) is a thiazole phenoxyacetic acid derivative and a selective agonist at peroxisome proliferator-activated receptor δ (PPARδ, also written PPARβ/δ), a fatty-acid-sensing nuclear receptor abundantly expressed in skeletal muscle. It is supplied as a reference standard for laboratory work on lipid catabolism, mitochondrial gene programmes and nuclear receptor selectivity.
Mechanism of Action & Research Context
PPARδ is a ligand-activated transcription factor. Its role is most clearly separated from the other PPAR subtypes by comparing agonists side by side in the same cell background.
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Lipid catabolism gene programme. In skeletal muscle cells, GW-501516 induces genes governing preferential lipid utilisation, β-oxidation, cholesterol efflux and energy uncoupling, and increases apolipoprotein-A1-specific efflux of intracellular cholesterol. The PPAR-dependent reporter in the muscle carnitine palmitoyltransferase-1 promoter is directly regulated by PPARβ/δ and not PPARα, in a PGC-1-dependent manner.[1]
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Subtype division of labour. In the same system, a PPARα agonist instead induces genes for fructose uptake and glycogen formation, and a PPARγ agonist induces glucose uptake, fatty acid synthesis and lipid storage. The three subtypes drive distinct and partly opposing programmes.[1]
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Fatty acid oxidation is not glucose handling. This distinction is where the compound is most often overstated. In L6 myotubes GW-501516 raises PGC-1α and CPT-1 expression and stimulates fatty acid oxidation, yet fails to enhance insulin sensitivity, AMPK activity, or glucose uptake and storage. The authors explicitly exclude sarcolemmal glucose transport as a target of PPARδ agonism in skeletal muscle.[2]
Research Applications
Primary fields of in vitro laboratory investigation include:
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Nuclear receptor subtype selectivity panels comparing PPARα, β/δ and γ agonists in one cell background.[1]
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Transcriptional profiling of β-oxidation, uncoupling and cholesterol efflux gene sets.[1]
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Substrate-utilisation assays separating fatty acid oxidation from glucose uptake and insulin signalling.[2]
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Promoter and reporter work on PPAR response elements such as the muscle CPT-1 promoter.[1]
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Analytical method development for chromatographic and mass-spectrometric identification.
Analytical Documentation
Purity and identity vary by manufacturing lot. Kimera Chems does not publish a single fixed purity figure for this item; refer to the batch-specific Certificate of Analysis (COA) issued for the lot received, which reflects third-party analytical testing for that lot.
References
- Dressel U, Allen TL, Pippal JB, Rohde PR, Lau P, Muscat GEO. The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Mol Endocrinol. 2003;17(12):2477–2493. doi:10.1210/me.2003-0151
- Dimopoulos N, Watson M, Green C, Hundal HS. The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells. FEBS Lett. 2007;581(24):4743–4748. doi:10.1016/j.febslet.2007.08.072
Storage & Handling
Store at controlled room temperature. Keep tightly closed. Liquid formats: do not refrigerate or freeze. Cold storage may cause the solution to cloud or precipitate. If this occurs, return to room temperature and mix until clear.
Storage guidance is a house recommendation. Analytical documentation is per-lot release testing.
Related Research Compounds
Research Use Only Disclaimer: This product is labeled and sold "For Research Use Only - NOT FOR HUMAN CONSUMPTION." It is not a drug, dietary supplement, food, cosmetic, or medical device, and it is not approved by the FDA or any other regulator for human or veterinary use. It is supplied to approved account holders as a research chemical for laboratory use and must be handled in accordance with applicable law.
