产品
编 号：F745305
分子式：C30H32N6O4
分子量：540.61
分子式：C30H32N6O4
分子量：540.61
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1448874-96-1
产品详情
生物活性：
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
体内研究：
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.Animal Model:8-10 weeks TGFβ positive female mice
Dosage:25 mg/kg
Administration:Oral administration; twice a day; 4 weeks
Result:Reduced lung fibrosis score, lung hydroxyproline levels and αSMA, a marker of early pulmonary fibrosis.
Animal Model:TNBS-induced IBD/acute colitis male CD-1 mice
Dosage:5, 15, 45 mg/kg
Administration:Oral administration; twice a day; 4 days
Result:Improved colonic histology and reduced the TNBS-induced loss of cupped cells at 15 mg/kg and 45 mg/kg significantly.Reduced the expression level of myeloperoxidase (MPO) at 5 mg/kg and 15 mg/kg significantly while there was no statistical difference at 45 mg/kg.
Animal Model:Male Sprague Dawley rats
Dosage:30 mg/kg
Administration:Intravenous injection; once
Result:The pharmacokinetic parameters of Ansornitinib (compound I)ParameterAnsornitinib (compound I)
t1/24.1 h
Tmax0.518 h
Cmax7860 ng/mL
Clearance173 mL/kg/min
steady-state volume18.2 L/kg
AUC0-last3180 ng/mL*h
AUC0?inf_obs3200 ng/mL*h
体外研究：
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.
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
体内研究：
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.Animal Model:8-10 weeks TGFβ positive female mice
Dosage:25 mg/kg
Administration:Oral administration; twice a day; 4 weeks
Result:Reduced lung fibrosis score, lung hydroxyproline levels and αSMA, a marker of early pulmonary fibrosis.
Animal Model:TNBS-induced IBD/acute colitis male CD-1 mice
Dosage:5, 15, 45 mg/kg
Administration:Oral administration; twice a day; 4 days
Result:Improved colonic histology and reduced the TNBS-induced loss of cupped cells at 15 mg/kg and 45 mg/kg significantly.Reduced the expression level of myeloperoxidase (MPO) at 5 mg/kg and 15 mg/kg significantly while there was no statistical difference at 45 mg/kg.
Animal Model:Male Sprague Dawley rats
Dosage:30 mg/kg
Administration:Intravenous injection; once
Result:The pharmacokinetic parameters of Ansornitinib (compound I)ParameterAnsornitinib (compound I)
t1/24.1 h
Tmax0.518 h
Cmax7860 ng/mL
Clearance173 mL/kg/min
steady-state volume18.2 L/kg
AUC0-last3180 ng/mL*h
AUC0?inf_obs3200 ng/mL*h
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备