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.

• 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]

• 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]

• 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:

• Nuclear receptor subtype selectivity panels comparing PPARα, β/δ and γ agonists in one cell background.^[1]

• Transcriptional profiling of β-oxidation, uncoupling and cholesterol efflux gene sets.^[1]

• Substrate-utilisation assays separating fatty acid oxidation from glucose uptake and insulin signalling.^[2]

• Promoter and reporter work on PPAR response elements such as the muscle CPT-1 promoter.^[1]

• 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.

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.