| 货号 | 16255-1mg |
| 描述 | GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).1 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.1 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.2,3,4 GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.5 Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gellibert, F.,de Gouville, A.C.,Woolven, J., et al. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): A potent, selective, and orally active transforming growth factor-β type I receptor inhibitor. Journal of Medicinal Chemistry 49, 2210-2221 (2006). 2.Lagares, D.,García-Fernández, R.A.,Jiménez, C.L., et al. Endothelin 1 contributes to the effect of transforming growth factor β1 on wound repair and skin fibrosis. Arthritis and Rheumatism 62(3), 878-889 (2010). 3.Tan, S.M.,Zhang, Y.,Connelly, K.A., et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. American Journal of Physiology.Heart and Circulatory Physiology 298(5), H1415-H1425 (2010). 4.de Oliveira, F.L.,Araújo-Jorge, T.C.,de Souza, E.M., et al. Oral administration of GW788388, an inhibitor of transforming growth factorβsignaling, prevents heart fibrosis in Chagas disease. PLoS Negl.Trop.Dis. 6(6), 1-14 (2012). 5.Noma, K.,Smalley, K.S.M.,Lioni, M., et al. The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis. Gastroenterology 134(7), 1981-1993 (2008). 6.Frazier, K.,Thomas, R.,Scicchitano, M., et al. Inhibition of ALK5 signaling induces physeal dysplasia in rats. Toxicologic Pathology 35(2), 284-295 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 425.5 |
| 分子式 | C25H23N5O2 |
| CAS号 | 452342-67-5 |
| 稳定性 | ≥ 2 years |
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