Discovery of Highly Potent Liver X Receptor 尾 Agonists was written by Kick, Ellen K.;Busch, Brett B.;Martin, Richard;Stevens, William C.;Bollu, Venkataiah;Xie, Yinong;Boren, Brant C.;Nyman, Michael C.;Nanao, Max H.;Nguyen, Lam;Plonowski, Artur;Schulman, Ira G.;Yan, Grace;Zhang, Huiping;Hou, Xiaoping;Valente, Meriah N.;Narayanan, Rangaraj;Behnia, Kamelia;Rodrigues, A. David;Brock, Barry;Smalley, James;Cantor, Glenn H.;Lupisella, John;Sleph, Paul;Grimm, Denise;Ostrowski, Jacek;Wexler, Ruth R.;Kirchgessner, Todd;Mohan, Raju. And the article was included in ACS Medicinal Chemistry Letters in 2016.COA of Formula: C8H5ClFN This article mentions the following:
Introducing a uniquely substituted Ph sulfone into a series of biphenyl imidazole liver X receptor (LXR) agonists afforded a dramatic potency improvement for induction of ATP binding cassette transporters, ABCA1 and ABCG1, in human whole blood. The agonist series demonstrated robust LXR尾 activity (>70%) with low partial LXR伪 agonist activity (<25%) in cell assays, providing a window between desired blood cell ABCG1 gene induction in cynomolgus monkeys and modest elevation of plasma triglycerides for agonist I. The addition of polarity to the Ph sulfone also reduced binding to the plasma protein, human 伪-1-acid glycoprotein. Agonist I was selected for clin. development based on the favorable combination of in vitro properties, excellent pharmacokinetic parameters and a favorable lipid profile. In the experiment, the researchers used many compounds, for example, 2-Chloro-6-fluorophenylacetonitrile (cas: 75279-55-9COA of Formula: C8H5ClFN).
2-Chloro-6-fluorophenylacetonitrile (cas: 75279-55-9) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.COA of Formula: C8H5ClFN
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics