Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (3R)-1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-3-piperidinecarboxylic acid
Purity: ≥98%
Formula Markup: C25H27FN6O4
Formula Weight: 494.518323
CAS Number: 2041073-22-5
Notes: A Dyrk1a and Gsk3ß inhibitor (IC50s = 6 and 16 nM, respectively, for the mouse enzymes); selective for Dyrk1a and Gsk3ß over a panel of 57 kinases but does inhibit 10 other kinases at 1 µM; increases the proliferation of R7T1 mouse pancreatic ß-cells and primary human pancreatic ß-cells (EC50s = 0.66 and 0.54 µM, respectively); increases the number of islet and ß-cells and the levels of total DNA and ATP in primary human islet cells at 2 µM; increases the proliferation of transplanted primary human islet cells and decreases the levels of blood glucose in mice at 50 mg/kg twice per day; reduces the levels of blood glucose in an OGTT in a transgenic RIP-DTA mouse model of type I diabetes at 50 mg/kg twice per day; increases the mass of, and levels of insulin in, pancreatic ß-cells in the same mice
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