TGFβ1-IN-1

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. In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Liver fibrosis C57BL/6J mice induced by CCl 4 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. Form:Solid

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