Zhang, Lei published the artcileA multiplexed cell assay in HepG2 cells for the identification of Δ5, Δ6, and Δ9 desaturase and elongase inhibitors, Related Products of piperazines, the publication is Journal of Biomolecular Screening (2010), 15(2), 169-176, database is CAplus and MEDLINE.
A multiplexed cell assay has been optimized to measure the activities of fatty acyl-CoA elongase, Δ5 desaturase (Δ5D), Δ6 desaturase (Δ6D), and Δ9 desaturase (Δ9D) together using 14C-labeled tracers in HepG2 cells, which express the human stearoyl-CoA desaturase-1 isoform (SCD1) exclusively. The Δ5 and Δ9 desaturase activities are indexed by the efficient conversion of [1-14C]-eicosatrienoic acid (C20:3, cis-8,11,14) to 14C-arachidonic acid (C20:4, cis-5,8,11,14) and the conversion of [1-14C]-stearic acid to 14C-oleic acid (C18:1, cis-9), resp. CP-74006 potently blocks the Δ5D activity with an IC50 value of 20 nM and simplifies the metabolism of [1-14C]-α-linolenate (C18:3, cis-9,12,15) by accumulating 14C-eicosatetraenoic acid (C20:4, cis-8,11,14,17) as the major 14C-eicosatrienoic acid (C20:3, cis-11,14,17) and 14C-docosatetraenoic acid (C22:4, cis-10,13,16,19) as the minor metabolites through Δ6 desaturation and elongation. This simplified metabolite spectrum enables the delineation of the Δ6D activity by comparing the combined Δ6D/elongase activity index of the 14C-(C20:4/C18:3) ratio with the corresponding elongation index of the 14C-(C20:3/C18:3) ratio following compound treatment. SC-26196 and sterculic acid specifically inhibit the Δ6D and Δ9D activities with an IC50 value of 0.1 μM and 0.9 μM, resp. This medium-throughput cell assay provides an efficient tool in the identification of specific desaturase and elongase inhibitors.
Journal of Biomolecular Screening published new progress about 218136-59-5. 218136-59-5 belongs to piperazines, auxiliary class Metabolic Enzyme,D6D, name is 2,2-Diphenyl-5-(4-((pyridin-3-ylmethylene)amino)piperazin-1-yl)pentanenitrile, and the molecular formula is C8H8O2, Related Products of piperazines.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics