On October 20, 2015, Caraballo, Remi; Larsson, Mikael; Nilsson, Stefan K.; Ericsson, Madelene; Qian, Weixing; Nguyen Tran, Nam Phuong; Kindahl, Tomas; Svensson, Richard; Saar, Valeria; Artursson, Per; Olivecrona, Gunilla; Enquist, Per-Anders; Elofsson, Mikael published an article.Recommanded Product: 99-60-5 The title of the article was Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo. And the article contained the following:
The risk of cardiovascular events increases in individuals with elevated plasma triglyceride (TG) levels, therefore advocating the need for efficient TG-lowering drugs. In the blood circulation, TG levels are regulated by lipoprotein lipase (LPL), an unstable enzyme that is only active as a non-covalently associated homodimer. We recently reported on a N-phenylphthalimide derivative (1) that stabilizes LPL in vitro, and moderately lowers triglycerides in vivo (Biochem. Biophys. Res. Commun.2014, 450, 1063). Herein, we establish structure-activity relationships of 51 N-phenylphthalimide analogs of the screening hit 1. In vitro evaluation highlighted that modifications on the phthalimide moiety were not tolerated and that lipophilic substituents on the central Ph ring were functionally essential. The substitution pattern on the central Ph ring also proved important to stabilize LPL. However, in vitro testing demonstrated rapid degradation of the phthalimide fragment in plasma which was addressed by replacing the phthalimide scaffold with other heterocyclic fragments. The in vitro potency was retained or improved and substance 80 proved stable in plasma and efficiently lowered plasma TGs in vivo. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Recommanded Product: 99-60-5
The Article related to structure preparation lipoprotein lipase agonist triglyceride, agonist, lpl, lipoprotein lipase, structure–activity relationship, triglyceride, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 99-60-5
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