AZ12799734

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZ12799734 (AZ-12799734) 是一种泛 BMP/TGFβ 抑制剂，可有效抑制配体激活的 SMAD3/4 转录，IC50 为 47 nM。

AZ12799734 (AZ-12799734) is a pan BMP/TGFβ inhibitor that potently inhibits ligand activated SMAD3/4 transcription with IC50 of 47 nM, inhibits receptor-mediated phosphorylation of SMAD1 by ALK1, BMPR1A and BMPR1B and phosphorylation of SMAD2 by ALK4, TGFBR1 and ALK7; inhibits TGFβ-induced migration in HaCaT cells.

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. Western Blot Analysis 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 Cell Line:HaCaT epithelial cells Concentration:500 nM Incubation Time:36 h Result:A dose-dependent decrease in TGFβ-induced migration was observed.

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 miceDosage: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.

AZ-12799734 | AZ 12799734

TGF-beta/Smad

TGFBR

TGFBR

——

——

1117684-36-2

370.427

C18H18N4O3S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (337.45 mM)

CC1=NC(=C(C=C1)OC2=CC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)N)C

4-((4-((2,6-dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years