Chemical Property of 4-(4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide
Chemical Property:
- PSA：92.79000
- Density:1.34
- LogP:4.50040
- Storage Temp.:2-8°C
- Solubility.:Soluble in DMSO (18 mg/ml with warming)
- XLogP3:2.7
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:5
- Exact Mass:425.18517499
- Heavy Atom Count:32
- Complexity:605
- Purity/Quality:
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99%, *data from raw suppliers
GW788388 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1COCCC1NC(=O)C2=CC=C(C=C2)C3=NC=CC(=C3)C4=C(NN=C4)C5=CC=CC=N5
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Description
GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) 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-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. GW 788388 also blocks TGF-β-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.
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Uses
GW788388 is a new TGF-beta type I receptor inhibitor with a much improved pharmacokinetic profile compared with SB431542.
