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AZ12799734
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZ12799734图片
CAS NO:1117684-36-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
AZ12799734 是一种选择性的、具有口服活性的TGFBR1激酶抑制剂,IC50为 47 nM。 AZ12799734 也是一种BMPTGFβ抑制剂。
生物活性

AZ12799734 is a selective, orally activeTGFBR1kinase inhibitor with anIC50of 47 nM. AZ12799734 is also a panBMPandTGFβinhibitor[1].

IC50& Target

TGFBR1

47 nM (IC50)

ALK6

0.017 μM (Kd)

ALK5

0.74 μM (Kd)

ALK4

1 μM (Kd)

ACVR1

6.2 μM (Kd)

ALK1

7.1 μM (Kd)

BMPR1A

40 μM (Kd)

BMP

 

体外研究
(In Vitro)

AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].
AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].
AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1].

Western Blot Analysis[1]

Cell Line:HaCaT cells and NIH3T3 cells
Concentration:10 nM
Incubation Time:10 days (HaCaT) or 24 h (NIH3T3)
Result:Blocked TGFβ-mediated induction of SMAD2 phosphorylation. Inhibited phosphorylation of both SMAD1 and SMAD2.

Cell Migration Assay[1]

Cell Line:HaCaT epithelial cells
Concentration:500 nM
Incubation Time:36 h
Result:A dose-dependent decrease in TGFβ-induced migration was observed.
体内研究
(In Vivo)

AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50of 0.01885 μM[1].

Animal Model:Ten-week-old female HsdHan:WIST rats[2]
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[1]
Dosage:50 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50of 0.01885 μM.
分子量

370.43

Formula

C18H18N4O3S

CAS 号

1117684-36-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.