Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 1-[2-(5-chloro-2-fluorophenyl)-5-methyl-4-pyridinyl]-1,2-dihydro-2-oxo-3H-imidazo[4,5-c]pyridine-3-acetamide
Purity: ≥95%
Formula Markup: C20H15ClFN5O2
Formula Weight: 411.8
CAS Number: 1976038-41-1
Notes: TP-008 is an inhibitor of activin receptor-like kinase 4 (ALK4) and ALK5, also known as TGF-β receptor type 1 (TGF-βRI; IC50s = 113 and 343 nM, respectively).{69894} It is selective for ALK4 and ALK5 over a panel of 467 kinases at 1 µM. TP-008 inhibits ALK4 or ALK5 signaling in a reporter assay using HEK293 cells expressing ALK4 or ALK5 (IC50s = 526 and 245 nM, respectively). It inhibits TGF-β1-induced increases in the levels of phosphorylated Smad2 in C2C12 mouse skeletal muscle myoblasts when used at concentrations of 1 or 10 µM. In vivo, TP-008 (150 or 500 mg/kg per day) induces valvular interstitial cell proliferation, neutrophil infiltration, hemorrhage, and fibrin deposition in rat heart valves.{69895}
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