产品
编 号：F039516
分子式：C18H18N4O3S
分子量：370.43
分子式：C18H18N4O3S
分子量：370.43
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
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1117684-36-2
产品详情
生物活性：
AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.
体内研究：
AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat.AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM.Animal Model:Ten-week-old female HsdHan:WIST rats
Dosage:200 and 400 mg/kg/day
Administration:Oral, 3-7 days
Result:Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage. Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.
Animal Model:Female BALB/c mice
Dosage:50 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
体外研究：
AZ12799734 inhibits ligand activated SMAD3/4 transcription.AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2.AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells.
AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.
体内研究：
AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat.AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM.Animal Model:Ten-week-old female HsdHan:WIST rats
Dosage:200 and 400 mg/kg/day
Administration:Oral, 3-7 days
Result:Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage. Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.
Animal Model:Female BALB/c mice
Dosage:50 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
体外研究：
AZ12799734 inhibits ligand activated SMAD3/4 transcription.AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2.AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells.
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