GW788388
Cat. No.：YN460002
CAS No. ：452342-67-5
| 产品名称: | GW788388 |
| CAS No.: | 452342-67-5 |
| Chemical Name: | 4-[4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide |
| Synonyms: | GW 788388 |
| 分子量: | 425.48 |
| 分子式: | C₂₅H₂₃N₅O₂ |
| SMILES: | O=C(C1=CC=C(C=C1)C2=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C2)NC5CCOCC5 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | GW788388 是一种有效的ALK5抑制剂，IC50值 18 nM；同时抑制 TGF-β II 型受体 和激活素 II 型受体的活性，但对 BMP II 型受体无作用。 |
| IC50和靶点: | |
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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 inhibitorJ. Med. Chem.49,2210-2221(2006)
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 fibrosisArthritis Rheum.62(3),878-889(2010)
Tan, S.M., Zhang, Y., Connelly, K.A., et al.Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarctionAm. J. Physiol. Heart Circ. Physiol.298(5),H1415-H1425(2010)
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 diseasePLoS Negl. Trop. Dis.6(6),1-14(2012)
Noma, K., Smalley, K.S.M., Lioni, M., et al.The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesisGastroenterology134(7),1981-1993(2008)
Frazier, K., Thomas, R., Scicchitano, M., et al.Inhibition of ALK5 signaling induces physeal dysplasia in ratsToxicol. Pathol.35(2),284-295(2014)
