In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. 766-11-0, formula is C5H3BrFN, Name is 5-Bromo-2-fluoropyridine. For this reason, pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Related Products of 766-11-0.
Bernard-Gauthier, Vadim;Mossine, Andrew V.;Knight, Ashley;Patnaik, Debasis;Zhao, Wen-Ning;Cheng, Chialin;Krishnan, Hema S.;Xuan, Lucius L.;Chindavong, Peter S.;Reis, Surya A.;Chen, Jinshan Michael;Shao, Xia;Stauff, Jenelle;Arteaga, Janna;Sherman, Phillip;Salem, Nicolas;Bonsall, David;Amaral, Brenda;Varlow, Cassis;Wells, Lisa;Martarello, Laurent;Patel, Shil;Liang, Steven H.;Kurumbail, Ravi G.;Haggarty, Stephen J.;Scott, Peter J. H.;Vasdev, Neil research published 《 Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery》, the research content is summarized as follows. Using structure-guided design, several cell based assays, and microdosed positron emission tomog. (PET) imaging, we identified a series of highly potent, selective and brain penetrant oxazole-4-carboxamide-based inhibitors of glycogen synthase kinase-3 (GSK-3). An isotopolog of our first-generation lead, [3H]PF-367, demonstrates selective and specific target engagement in vitro, irresp. of activation state. We discovered substantial ubiquitous GSK-3-specific radioligand binding in Tg2576 Alzheimer’s disease (AD), suggesting application for these compounds in AD diagnosis, and identified [11C]OCM-44 as our lead GSK-3 radiotracer, with optimized brain uptake by PET imaging in nonhuman primates. GSK-3β-isoenzyme selectivity was assessed to reveal OCM-51, the most potent (IC50 = 0.030 nM) and selective (>10-fold GSK-3β/GSK-3α) GSK-3β inhibitor known to date. Inhibition of CRMP2T514 and tau phosphorylation, as well as favorable therapeutic window against WNT/β-catenin signaling activation was observed in cells.
766-11-0, 5-Bromo-2-fluoropyridine is a useful research compound. Its molecular formula is C5H3BrFN and its molecular weight is 175.99 g/mol. The purity is usually 95%.
5-Bromo-2-fluoropyridine is a boronic acid that has been shown to react with iodides and form 5-bromo-2-fluoroiodobenzene. The reaction of 5-bromo-2-fluoropyridine with benzene gives the same product as the reaction with 1,3,5-trioxane. The UV absorption of 5-bromo-2-fluoropyridine is found at 230 nm and 260 nm. It also has an absorption band in the infrared region at 1625 cm−1. Vibrational progressions have been observed for this molecule, which are due to dipole moments and electron density distributions in the molecule.
5-bromo-2-fluoropyridine is used in the synthesis of heteroaromatic and aniline derivatives of piperidines as potent ligands used for vesicular acetylcholine transport. , Related Products of 766-11-0