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CAS No. : 1448874-96-1
MCE 国际站:Ansornitinib
产品活性:Ansornitinib 是一种具有口服活性的双激酶抑制剂,可以抑制血小板衍生生长因子受体 (PDGFR) 和血管内皮生长因子受体 (VEGFR2)。Ansornitinib 可作为一种抗纤维化剂,用于肺部,肝脏,肾脏以及胃肠等纤维化疾病的研究。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:VEGFR | PDGFR
In Vitro: Ansornitinib (compound I) (0.1 nM-10 μM, 2 h) can significantly inhibit the phosphorylation of PDGFRβ in human hepatic stellate cells and KDR phosphorylation in human umbilical vein endothelial cells (HUVEC).
Ansornitinib (compound I) (0.1-13 μM, 48 h) can induce a decrease in the expression of many different inflammation-related markers, such as macrophage colony-stimulating factor (M-CSF), soluble interleukin 8, and fibrosis-related markers, such as N-calmodulin, α-SMA, etc., in a dose-dependent manner.
In Vivo: Ansornitinib (compound I) (25 mg/kg, p.o., twice a day, 4 weeks) can reduce fibrosis in TGFβ positive female mice.
Ansornitinib (compound I) (5-45 mg/kg, p.o., twice a day, 4 days) can reduce inflammatory bowel disease (IBD) in TNBS-induced IBD/acute colitis male CD-1 mice.
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