Related Products of 403-33-8In 2021 ,《Second-Generation Dual FXR/sEH Modulators with Optimized Pharmacokinetics》 was published in Journal of Medicinal Chemistry. The article was written by Helmstaedter, Moritz; Kaiser, Astrid; Brunst, Steffen; Schmidt, Jurema; Ronchetti, Riccardo; Weizel, Lilia; Proschak, Ewgenij; Merk, Daniel. The article contains the following contents:
Non-alc. steatohepatitis (NASH) presents as an epidemic chronic liver disease that is closely associated with metabolic disorders and involves hepatic steatosis, inflammation, and fibrosis as key factors. Despite the enormous global prevalence of NASH, effective pharmacol. interventions are lacking. Based on the hypothesis that the multifactorial condition NASH may benefit from combined multiple modes of action for enhanced therapeutic efficacy, we have previously developed dual FXR activators/sEH inhibitors (FXRa/sEHi) and observed remarkable antifibrotic effects upon their use in rodent NASH models. However, these first-generation FXRa/sEHi were characterized by moderate metabolic stability and short in vivo half-life. Aiming to overcome these pharmacokinetic drawbacks, we have systematically studied the structure-activity and structure-stability relationships of the chemotype and obtained second-generation FXRa/sEHi with improved pharmacokinetic parameters. With high plasma exposure, a half-life greater than 5 h, and similar dual potency on the intended targets, I presents as a substantially optimized FXRa/sEHi for late-stage preclin. development.Methyl 4-fluorobenzoate(cas: 403-33-8Related Products of 403-33-8) was used in this study.
Methyl 4-fluorobenzoate(cas: 403-33-8) can be used in the synthesis of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH2-substituted benzyl moiety.Related Products of 403-33-8
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