产品
编 号：F494660
分子式：C20H18FN5O
分子量：363.39
分子式：C20H18FN5O
分子量：363.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 879487-87-3
产品详情
生物活性：
R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
体内研究：
R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC0-24 values of 0.075, 0.28, 1.6 and 8.2 μg?h/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively.R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model.R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg.Animal Model:Male WKY/Hos rats.
Dosage:0.3, 1, 3, and 10 mg/kg
Administration:Oral administration; single.
Result:1.19Pharmacokinetic Parameters of R-268712 in male WKY/Hos rats (n=4).PO (0.3 mg/kg)PO (1 mg/kg)PO (3 mg/kg)PO (10 mg/kg)
AUC0-24 (μg?h/mL)0.0750.281.68.2
Animal Model:Male Col1a1-Luc Tg rats (10 to14-week-old; UUO model; n=5-6).
Dosage:1, 3, 10 mg/kg
Administration:Oral administration; single daily for 3 days.
Result:Suppressed activity of renal luciferase in a dose-dependent manner.
Animal Model:Male WKY/Hos rats (4-week-old; Thy1 nephritis model; n=7).
Dosage:0.3, 1 mg/kg
Administration:Oral administration; single daily for 33 days.
Result:Significantly reduced proteinuria at day 21( the repression continued until day 28), and serum creatinine level (dosage at 1 mg/kg).Apparently suppressed glomerular sclerosis by 28% and reduced the increase of the hydroxyproline content when at 1 mg/kg.Suppressed the activation of mesangial parenchymal cell and the injury of podocyte on the basis of TGF-β signaling inhibition at 1 mg/kg.
体外研究：
R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM in HFL-1 cells.R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells.
R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
体内研究：
R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC0-24 values of 0.075, 0.28, 1.6 and 8.2 μg?h/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively.R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model.R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg.Animal Model:Male WKY/Hos rats.
Dosage:0.3, 1, 3, and 10 mg/kg
Administration:Oral administration; single.
Result:1.19Pharmacokinetic Parameters of R-268712 in male WKY/Hos rats (n=4).PO (0.3 mg/kg)PO (1 mg/kg)PO (3 mg/kg)PO (10 mg/kg)
AUC0-24 (μg?h/mL)0.0750.281.68.2
Animal Model:Male Col1a1-Luc Tg rats (10 to14-week-old; UUO model; n=5-6).
Dosage:1, 3, 10 mg/kg
Administration:Oral administration; single daily for 3 days.
Result:Suppressed activity of renal luciferase in a dose-dependent manner.
Animal Model:Male WKY/Hos rats (4-week-old; Thy1 nephritis model; n=7).
Dosage:0.3, 1 mg/kg
Administration:Oral administration; single daily for 33 days.
Result:Significantly reduced proteinuria at day 21( the repression continued until day 28), and serum creatinine level (dosage at 1 mg/kg).Apparently suppressed glomerular sclerosis by 28% and reduced the increase of the hydroxyproline content when at 1 mg/kg.Suppressed the activation of mesangial parenchymal cell and the injury of podocyte on the basis of TGF-β signaling inhibition at 1 mg/kg.
体外研究：
R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM in HFL-1 cells.R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells.
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