GW 788388

GW 788388 is a selective inhibitor of transforming growth factor-beta (TGF-beta) type 1 receptor (TGFBR1 or ALK5, IC50 = 18 nM). 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. As TGF-beta stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of alpha-smooth muscle actin and production of collagen I. GW 788388 also blocks TGF-beta-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro. Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.Formal Name: 4-[4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide. CAS Number: 452342-67-5. Molecular Formula: C25H23N5O2. Formula Weight: 425.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 261 nm. SMILES: O=C(C1=CC=C(C2=NC=CC(C3=CNN=C3C4=CC=CC=N4)=C2)C=C1)NC5CCOCC5. InChi Code: InChI=1S/C25H23N5O2/c31-25(29-20-9-13-32-14-10-20)18-6-4-17(5-7-18)23-15-19(8-12-27-23)21-16-28-30-24(21)22-3-1-2-11-26-22/h1-8,11-12,15-16,20H,9-10,13-14H2,(H,28,30)(H,29,31). InChi Key: SAGZIBJAQGBRQA-UHFFFAOYSA-N.