265129-69-9

Upstream product

• 1402394-03-9 tert-butyl 2-(4-chloromethylphenylthio)-2-methylpropanoate 
• 1402394-02-8 tert-butyl 2-(4-hydroxymethylphenylthio)-2-methylpropanoate 
• 60439-16-9 1-bromo-4-cyclohexylbutane 
• 247923-33-7 1,1-dimethylethyl 2-[[4-(2-aminoethyl)phenyl]thio]-2-methyl-propanoate 
• 53339-53-0 4-mercaptobenzyl alcohol 
• 1074-36-8 4-mercaptobenzoic acid 

Downstream Products

• 1402393-99-0 C₃₄H₅₀N₂O₄S 
• 1402394-00-6 C₃₄H₅₀N₂O₄S 
• 1402394-01-7 C₃₄H₅₀N₂O₄S 

Relevant academic research and scientific papers

Synthesis, radiolabeling and initial in vivo evaluation of [ 11C]KSM-01 for imaging PPAR-α receptors

Peroxisome proliferator-activated receptor alpha (PPAR-α) is a ligand-activated nuclear receptor transcription factor that regulates the fatty acid β-oxidation. An in vitro assay identified the p-methoxy phenyl ureido thiobutyric acid derivative KSM-01 (IC50 = 0.28 ± 0.09 nM) having a higher affinity to activate PPAR-α than the PPAR-α agonist GW7647 (IC50 = 0.46 ± 0.19 nM). In this study, we report the synthesis and initial in vivo evaluation of [11C]KSM-01. The radiosynthesis was carried out by first alkylating the corresponding p-phenol precursor with [11C]MeI in DMF using NaOH, followed by deprotection of the t-butyl ester group by TFA, yielding [11C]KSM-01. SUV analysis of dynamic micro PET/CT imaging data showed that [11C]KSM-01 accumulation was ～2.0-fold greater in cardiac-specific PPAR-α overexpressing transgenic mice compared to wild-type littermates. The post-PET biodistribution studies were consistent with these results and demonstrated 2.5-fold greater radiotracer uptake in the heart of transgenic mice compared to the wild-type littermates. These results demonstrate the potential utility of PPAR-α agonists as PET radiopharmaceuticals.