PPAR agonist 4 (Compound 12) is an orally available PPAR agonist that activates PPARα, PPARδ, and PPARγ with EC50 values of 0.7, 0.7, and 1.8 μM, respectively. PPAR agonist 4 has anti-fibrotic activity.

Physicochemical Properties

Molecular Formula	C23H28F3N3O3
Molecular Weight	451.48
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)

Biological Activity

Targets	PPARα 0.7 μM (EC50) PPARδ 0.7 μM (EC50) PPARγ 1.8 μM (EC50)
ln Vitro	PPAR agonist 4 (3-10 μM) dose-dependently upregulates the expression of PPARα/δ target genes CPT1A, PDK4, and ANGPTL4 in HepG2 cells, and PPARγ target genes CD36 and FABP4 in HEK293 cells [1].
ln Vivo	PPAR agonist 4 (3-30 mg/kg, oral, 3 weeks) can improve collagen deposition and inhibit inflammatory cell infiltration in a CCl4-induced liver fibrosis mouse model [1]. PPAR agonist 4 in SD rats
Cell Assay	RT-PCR[1] Cell Types: HepG2 and HEK293 Tested Tested Concentrations: 3-10 μM Incubation Duration: 12 h Experimental Results: Upregulated levels of CPT1A, PDK4 and ANGPTL4, downregulated levels of CD36 and FABP4.
Animal Protocol	Animal/Disease Models: CCL4-induced liver fibrosis in C57BL/6 mice[1] Doses: 3-30 mg/kg Route of Administration: p.o., once a day for 3 weeks Experimental Results: Reduced levels of collagen and α-SMA, reduced accumulation of collagen and inflammatory cell infiltration in the portal area. Upregulated the expression of PPARs target genes (Cpt1a, Cpt2, Angptl4 and Cd36).
References	[1]. Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis. Eur J Med Chem. 2024 Apr 5;269:116344.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2149 mL	11.0747 mL	22.1494 mL
	5 mM	0.4430 mL	2.2149 mL	4.4299 mL
	10 mM	0.2215 mL	1.1075 mL	2.2149 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.