PPARδ agonist 10 (compound 7) is an orally active, selective partial agonist of PPARδ with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assays but a full agonist of free fatty acid oxidation in muscle cells in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research.

Physicochemical Properties

Molecular Formula	C23H17BR2CLO3S
Molecular Weight	568.71
CAS #	685139-10-0
SMILES	C1=C(C=CC(=C1)Br)C(=CCSC2=CC(=C(C=C2)OCC(=O)O)Cl)C3=CC=C(C=C3)Br
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	PPARδ 0.053 μM (EC50, hPPARδ) PPARδ 0.30 μM (EC50, mPPARδ)
ln Vitro	PPARδ agonist 10 (compound 7) increases fatty acid oxidation in rat L6 myocytes with an EC50 of 30 nM[1].
ln Vivo	PPARδ agonist 10 (compound 7) changes plasma lipid parameters in a dose-dependent manner to reduce atherosclerosis[1]. PPARδ agonist 10 (5-20 mg/kg, oral, once daily) exhibits good oral pharmacokinetic properties in rats[1].
Animal Protocol	Animal/Disease Models: ApoB100/CETP-Tgn mice (female, 9-11 weeks old, with a mean body weight of 19.2 g±1.4, n=8/group, were fed a high fat diet)[1] Doses: 5, 10, and 20 mg/kg Route of Administration: PO, once daily, for 6 weeks Experimental Results: Changed plasma lipid parameters in a dose-dependent manner to a less atherogenic profile, with increased HDL and decreased LDL and TG. HbA1c levels were lowered. Animal/Disease Models: Male SD rats[1] Doses: 1.06 mg/kg (IV)/2.06 mg/kg (PO) Route of Administration: p.o. and i.v., single (Pharmacokinetic Analysis) Experimental Results: Pharmacokinetic Parameters of PPARδ agonist 10 in male Sprague-Dawley rats[1]. IV (1.06 mg/kg) PO (2.06 mg/kg) Cmax (ng/mL) 508 AUC0-24 (ng/mL∗min) 79294 t1/2 (min) 59 CL (mL/min/kg) 11.9 Vd, ss (L/kg) 0.3 F (%) 46%
References	[1]. Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo. J Med Chem. 2007 Apr 5;50(7):1495-503.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.7584 mL	8.7918 mL	17.5837 mL
	5 mM	0.3517 mL	1.7584 mL	3.5167 mL
	10 mM	0.1758 mL	0.8792 mL	1.7584 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.