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Discovery and Synthesis of a Direct Activator of AMP-Kinase PF-06409577 against Diabetic Nephropathy
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Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. PF-06409577 has been discovered as an indole acid with excellent balance of properties and has now been advanced to first-in-human trials for the treatment of diabetic nephropathy. Key indazoles in the synthesis were prepared by Suzuki coupling to some commercially available 5-bromoindazoles (scheme).
SiliaMetS Thiol was used to remove remaining Pd after only 30 min of stirring.
Cameron, K. et al. J. Med. Chem., 2016, 59, 8068 - 8081
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SiliaMetS Thiol (SH) Metal Scavenger (R51030B)
Our most versatile and robust metal scavenger for a variety of metals under a wide range of conditions. Best scavenger for: Ag, Hg, Os, Pd & Ru. Good scavenger for: Cu, Ir, Pb, Rh, Se & Sn.
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