Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 4-[4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
Purity: ≥98%
Formula Markup: C25H23N5O2
Formula Weight: 425.5
CAS Number: 452342-67-5
Notes: GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}
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