Wong, Siu Wai; Vivash, Lucy; Mudududdla, Ramesh; Nguyen, Nghi; Hermans, Stefan J.; Shackleford, David M.; Field, Judith; Xue, Lian; Aprico, Andrea; Hancock, Nancy C.; Haskali, Mohammad; Stashko, Michael A.; Frye, Stephen V.; Wang, Xiaodong; Binder, Michele D.; Ackermann, Uwe; Parker, Michael W.; Kilpatrick, Trevor J.; Baell, Jonathan B. published an article in 2021. The article was titled 《Development of [18F]MIPS15692, a radiotracer with in vitro proof-of-concept for the imaging of MER tyrosine kinase (MERTK) in neuroinflammatory disease》, and you may find the article in European Journal of Medicinal Chemistry.Application of 27489-62-9 The information in the text is summarized as follows:
MER tyrosine kinase (MERTK) upregulation is associated with M2 polarization of microglia, which plays a vital role in neuroregeneration following damage induced by neuroinflammatory diseases such as multiple sclerosis (MS). Therefore, a radiotracer specific for MERTK could be of great utility in the clin. management of MS, for the detection and differentiation of neuroregenerative and neurodegenerative processes. This study aimed to develop an [18F] ligand with high affinity and selectivity for MERTK as a potential positron emission tomog. (PET) radiotracer. MIPS15691 and MIPS15692 were synthesized and kinase assays were utilized to determine potency and selectivity for MERTK. Both compounds were shown to be potent against MERTK, with resp. IC50 values of 4.6 nM and 4.0 nM, and were also MERTK-selective. Plasma and brain pharmacokinetics were measured in mice and led to selection of MIPS15692 over MIPS15691. X-ray crystallog. was used to visualize how MIPS15692 is recognized by the enzyme. [18F]MIPS15692 was synthesized using an automated iPHASE FlexLab module, with a molar activity (Am) of 49 ± 26 GBq/μmol. The radiochem. purity of [18F]MIPS15692 was >99% and the decay-corrected radiochem. yields (RCYs) were determined as 2.45 ± 0.85%. Brain MERTK protein d. was measured by a saturation binding assay in the brain slices of a cuprizone mouse model of MS. High levels of specific binding of [18F]MIPS15692 to MERTK were found, especially in the corpus callosum/hippocampus (CC/HC). The in vivo PET imaging study of [18F]MIPS15692 suggested that its neuroPK is sub-optimal for clin. use. Current efforts are underway to optimize the neuroPK of our next generation PET radiotracers for maximal in vivo utility. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Application of 27489-62-9
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts