AZ12799734|cas:1117684-36-2|西域试剂

AZ12799734

产品编号：Bellancom-123900| CAS NO：1117684-36-2| 分子式：C₁₈H₁₈N₄O₃S| 分子量：370.43

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货号	价格	库存与货期
Bellancom-123900	￥1400.00	杭州北京（现货）
Bellancom-123900	￥2250.00	杭州北京（现货）
Bellancom-123900	￥4950.00	杭州北京（现货）
Bellancom-123900	￥8000.00	杭州北京（现货）

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AZ12799734

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 BMP 和 TGFβ 抑制剂。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.