Peroxisome proliferator-activated receptors which comprise three subtypes (PPAR alpha, deltaand gamma) have recently received significant attention due to their function as transcription factors that regulate gene expression patterns of biological processes. Among these subtypes, PPAR deltais related to various metabolic diseases. In this regard, diverse strategies for development of PPAR delta modulators have been widely studied. Recently, GlaxoSmithKline discovered highly potent and selective PPARdelta agonists such as GW501516 and GW610742. Based on these model compounds, several types of PPAR delta agonists have been devised. To this extent, GW501516 modified “Y”-shaped PPARdelta specific agonists were reported by Kang group. Evans group also reported new type of “Y”-shaped PPARdelta agonists. Based on these works, we designed and synthesized various “Y”-shaped biaryl PPARdelta agonists. Structure-activity relationship (SAR) analysis was performed to find title compound 1 that the most active agonist with an EC₅₀ of 2.6 nM. Activity of enantiospecific R and S isomers of compound 1 was confirmed that R isomer (EC₅₀ = 0.7 nM) shows much more potent activity than S isomer (EC₅₀ = 6.1 nM). Molecular docking studies between the PPAR ligand binding domain and enantiospecific R and S isomers of compound 1 were conducted. In vitro absorption, distribution, metabolism, excretion, and toxicity (ADMET) and in vivo PK profiles show that compound 1 involves reasonable drug-like properties and good bioavailability. Our overall results clearly demonstrate that this orally available PPAR delta agonist 1 is a viable drug candidate for the treatment of PPAR delta-related diseased.