GW-0742

GW-0742 (PPAR-δ Agonist)

GW-0742 (also designated GW-610742 or GW-0742X) is a synthetic small-molecule agonist of the peroxisome proliferator-activated receptor delta (PPAR-δ/β). Characterized in medicinal chemistry literature as one of the most potent and selective PPAR-δ ligands described to date, it exhibits high binding affinity with reported EC₅₀ values of approximately 1 nM at human PPAR-δ and approximately 1,000-fold selectivity over PPAR-α and PPAR-γ. It serves as a widely cited reference ligand in nuclear receptor signaling and lipid metabolism research.

Technical Specifications

Research Applications & Mechanism of Action

GW-0742 binds to the ligand-binding domain of PPAR-δ, inducing heterodimerization with the retinoid X receptor (RXR). This complex binds to peroxisome proliferator response elements (PPREs) in target gene promoters, modulating the transcription of genes involved in mitochondrial function, fatty acid uptake, fatty acid oxidation, and inflammatory signaling.

Primary fields of in vitro and preclinical laboratory investigation include:

• PPAR-δ Pathway Analysis: Mapping binding, transactivation, and downstream gene expression profiles.

• Lipid Metabolism: Investigating signaling pathways related to fatty acid oxidation.

• Tissue Protection Models: Utilizing the compound in cardiovascular, hepatic, and neuronal protection studies.

• Inflammatory Signaling: Examining PPAR-δ involvement in immune cell signaling.

• Selectivity Profiling: Conducting structure-activity relationship (SAR) analysis across PPAR subtypes.

Safety, Storage, & Handling

Toxicological Note: GW-0742 is part of a series of PPAR-δ agonists originally developed for pharmaceutical programs, which were subsequently discontinued from clinical development following long-term rodent carcinogenicity findings. This toxicology profile is a documented part of the scientific record and reinforces the strictly non-clinical, research-only application of this compound.

• Storage Guidelines: For long-term stability, store the material in dry, cool, light-protected conditions at -20 °C.

• Solubility: The compound is soluble in DMSO but demonstrates poor solubility in water.

Research Use Disclaimer

This product is developed and distributed strictly as a Research Use Only (RUO) laboratory reagent intended exclusively for non-clinical analytical and scientific investigation. It is not an FDA-approved drug formulation, clinical therapeutic, or diagnostic agent, and is strictly prohibited for human or veterinary consumption. Kimera Chems provides these high-purity chemical batches solely to accredited institutional laboratories and qualified scientific investigators.