Development of Gleevec Analogues for Reducing Production of 閻?Amyloid Peptides through Shifting 閻?Cleavage of Amyloid Precursor Proteins was written by Sun, Weilin;Netzer, William J.;Sinha, Anjana;Gindinova, Katherina;Chang, Emily;Sinha, Subhash C.. And the article was included in Journal of Medicinal Chemistry in 2019.SDS of cas: 162046-66-4 This article mentions the following:
Imatinib mesylate, I, inhibits production of 閻?amyloid (A閻? peptides both in cells and in animal models. It reduces both the 閻?secretase and 缂?secretase cleavages of the amyloid precursor protein (APP) and mediates a synergistic effect, when combined with a 閻?secretase inhibitor, BACE IV. Toward developing more potent brain-permeable leads, we have synthesized and evaluated over 75 I-analogs. Several compounds inhibited production of A閻?peptides with improved activity in cells. These compounds affected 閻?secretase cleavage of APP similarly to I. Compound II significantly reduced production of the A閻?2 peptide, when administered (100 mg/kg, twice daily by oral gavage) to 5 mo old female mice for 5 days. A combination of compound II with BACE IV also reduced A閻?levels in cells, more than the additive effect of the two compounds These results open a new avenue for developing treatments for Alzheimer’s disease using I-analogs. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4SDS of cas: 162046-66-4).
4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 闁硅櫣鐓?and boils at 125闂?30 闁硅櫣鐓? Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.SDS of cas: 162046-66-4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics