1. Product Overview
GW 6471 (CAS 880635-03-0), systematically named (S,Z)-N-(3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-((4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-en-2-yl)amino)propyl)propanamide, is a potent and selective antagonist of peroxisome proliferator-activated receptor alpha (PPARα). With the molecular formula C₃₅H₃₆F₃N₃O₄ and a molecular weight of 619.67 g/mol, it appears as a yellow to off-white powder at room temperature. GW 6471 inhibits PPARα activation with an IC₅₀ of 0.24 µM and functions by inducing a conformational change in PPARα that promotes the recruitment of corepressors, thereby blocking agonist-induced transcriptional activity. It is a critical pharmacological tool for dissecting lipid metabolism, glucose homeostasis, and PPARα-mediated signaling in oncology and metabolic disease research. This product is supplied exclusively for laboratory research use and is not intended for clinical, diagnostic, veterinary, food, or cosmetic applications.
2. Key Features and Advantages
• High potency and selectivity: Potent PPARα antagonist (IC₅₀ = 0.24 µM) with minimal activity against PPARγ and PPARδ at micromolar concentrations.
• Well-defined mechanism: Induces PPARα conformational shift to favor corepressor binding, effectively reversing agonist effects.
• High purity: Typically ≥98% by HPLC, suitable for cell-based reporter assays, gene expression analysis, and in vivo pharmacological studies.
• Good solubility: Readily soluble in DMSO (≥15 mg/mL), DMF, and DMSO:PBS (1:3) mixtures; enables convenient preparation of concentrated stock solutions.
• Consistent batch quality with supporting analytical data (HPLC, LC-MS, NMR) available from qualified suppliers; widely cited in studies on metabolic reprogramming and cancer biology.
• Stable under recommended storage conditions, ensuring reliable experimental outcomes across long-term research projects.
3. Main Applications
• Metabolic disease research: Investigating PPARα's role in fatty acid oxidation, lipid metabolism, insulin sensitivity, and hepatic steatosis models.
• Oncology studies: Evaluating PPARα inhibition effects on tumor cell proliferation, apoptosis, and metabolic rewiring in renal cell carcinoma, breast cancer, and other malignancies.
• Signaling pathway analysis: Probing crosstalk between PPARα and key oncogenic pathways such as PI3K/Akt/mTOR and NF-κB in inflammatory and proliferative contexts.
• Pharmacological tool for distinguishing PPARα-mediated effects from PPARγ/δ activities in complex biological systems.
• Medicinal chemistry reference: Used as a structural template for developing novel PPAR modulators with improved pharmacokinetic or selectivity profiles.
4. Technical Specifications
5. Storage and Handling
• Store the powdered compound sealed with desiccant, protected from light; recommended storage at -20°C (long term). For DMSO stock solutions, aliquot and store at -80°C to maximize stability; avoid repeated freeze–thaw cycles. Typical working stocks are 10–20 mM in anhydrous DMSO.
• Before opening, allow the sealed vial to warm to room temperature to prevent moisture condensation. Keep container tightly closed when not in use.
• Handle in a well-ventilated area or fume hood. Use personal protective equipment including safety glasses, nitrile gloves, and a lab coat. Avoid inhalation of dust and contact with skin or eyes.
• Intended exclusively for laboratory research by qualified personnel; not for human or veterinary use, food, drug, or cosmetic applications.
6. Safety Overview
• GW 6471 is a research chemical with limited toxicological data. Treat as potentially hazardous: may cause irritation to eyes, skin, and respiratory system.
• In case of eye contact, rinse immediately with plenty of running water for at least 15 minutes and seek medical advice. In case of skin contact, wash thoroughly with soap and water.
• If inhaled, move the person to fresh air and keep at rest in a position comfortable for breathing. If ingested, rinse mouth and seek medical attention—do not induce vomiting unless directed by medical personnel.
• Use appropriate engineering controls (fume hood) and personal protective equipment (safety goggles, nitrile gloves, lab coat). Avoid generating dust.
• Dispose of in accordance with local regulations for chemical waste. Do not discharge into drains, waterways, or soil.
• For detailed safety information, refer to the applicable Safety Data Sheet (SDS) prior to handling.
