Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable 纬-Secretase Modulator was written by Peng, Hairuo;Talreja, Tina;Xin, Zhili;Cuervo, J. Hernan;Kumaravel, Gnanasambandam;Humora, Michael J.;Xu, Lin;Rohde, Ellen;Gan, Lawrence;Jung, Mi-young;Shackett, Melanie N.;Chollate, Sowmya;Dunah, Anthone W.;Snodgrass-Belt, Pamela A.;Arnold, H. Moore;Taveras, Arthur G.;Rhodes, Kenneth J.;Scannevin, Robert H.. And the article was included in ACS Medicinal Chemistry Letters in 2011.Application of 4045-30-1 This article mentions the following:
We have investigated a novel series of acid-derived 纬-secretase modulators as a potential treatment of Alzheimer’s disease. Optimization based on cellular potency and brain pharmacodynamics after oral dosing led to the discovery of 10a (BIIB042). Compound 10a is a potent 纬-secretase modulator, which lowered A尾42, increased A尾38, but had little to no effect on A尾40 levels both in vitro and in vivo. In addition, compound 10a did not affect Notch signaling in our in vitro assessment. Compound 10a demonstrated excellent pharmacokinetic parameters in multiple species. Oral administration of 10a significantly reduced brain A尾42 levels in CF-1 mice and Fischer rats, as well as plasma A尾42 levels in cynomolgus monkeys. Compound 10a was selected as a candidate for preclin. safety evaluation. In the experiment, the researchers used many compounds, for example, 4,4-Dimethylpiperidine (cas: 4045-30-1Application of 4045-30-1).
4,4-Dimethylpiperidine (cas: 4045-30-1) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Application of 4045-30-1
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem