1047641-65-5

Upstream product

• 42558-54-3 Methyl 4-methyl-3-oxopentanoate 
• 1199-28-6 2-(2,4-dichlorophenoxy)ethylamine 
• 120-83-2 2,4-dichlorophenol 
• 870194-65-3 tert-butyl (2-(2,4-dichlorophenoxy)ethyl)carbamate 

Downstream Products

• 927187-53-9 (3-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-isopropyl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 
• 919283-75-3 (3-chloro-4-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-isopropyl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 

Relevant academic research and scientific papers

3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists: Part 1

We report the identification of a novel series of trisubstituted isoxazoles as PPAR activators from a high-throughput screen. A series of structural optimizations led to improved efficacy and excellent functional receptor selectivity for PPARδ. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif.

3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists. Part 2

A series of PPARδ-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARδ agonist with good in vivo PK properties in mouse (Cmax = 5.1 μM, t1/2 = 3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARδ is discussed.