TGFβ1-IN-1 (compound 42) 是一种有效的、具有口服活性的TGF-β1抑制剂。TGFβ1-IN-1 可以抑制 TGF-β1 诱导的纤维化标志物（α-SMA 和纤连蛋白）的上调，可用于肝纤维化疾病研究。

TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies [1].

TGFβ1-IN-1 (compound 42) (0-20 μM, 72 h) inhibits the proliferation of TGF-β1 (5 ng/mL)-treated LX- 2 cells and inhibits LO2 cell viability with an IC 50 of 105 μM [1]. Cell Viability Assay [1] Cell Line: HSCs (LX-2) cells Concentration: 20 μM Incubation Time: 24 or 72 hours Result: Showed the survival rate of 77.5% and the inhibition rate of 30.3% for LX-2 cells. Significantly inhibited fibronectin and α-SMA protein expression.

TGFβ1-IN-1 (compound 42) (p.o., 15 or 30 mg/kg, daily, 3weeks) prevents CCl 4 -induced liver injury and fibrosis, inhibits the activation of hepatic stellate cell (HSC) and epithelial-mesenchymal transition (EMT), and improves the immune microenvironment of CCl 4 -induced liver fibrosis as well as CCl 4 -induced systemic toxicity in C57BL/6J mice [1]. Animal Model: Liver fibrosis C57BL/6J mice induced by CCl 4 [1] Dosage: 15 or 30 mg/kg Administration: Oral administration; daily; 3 weeks Result: Significantly prevented CCl 4 -induced liver injury and reduced liver weight factor, serum ALT, AST, CHO and TG levels. Significantly improved structural damage and inflammatory cell infiltration in the liver, and reduced collagen deposition in liver tissue. Reduced accumulation of CCl 4 -induced immune cells, such as hepatic macrophages (F4/80 + CD11b + ), Th1 cells (CD69 + CD4 + ), and Th2 cells (CD69 + CD8 + ) so on.

C22H24N2O3

364.44

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years