TGFβ1-IN-1

Research use only, not for human use.

TGFβ1-IN-1 is an orally active TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrotic markers (α-SMA and fibronectin) and can be used for the study of cancer and autoimmune diseases.

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.

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.Cell Viability Assay 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 CCl4-induced liver injury and fibrosis, inhibits the activation of hepatic stellate cell (HSC) and epithelial-mesenchymal transition (EMT), and improves the immune microenvironment of CCl4-induced liver fibrosis as well as CCl4-induced systemic toxicity in C57BL/6J mice.Animal Model:Liver fibrosis C57BL/6J mice induced by CCl4 Dosage:15 or 30 mg/kg Administration: Oral administration; daily; 3 weeks Result:Significantly prevented CCl4-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 CCl4-induced immune cells, such as hepatic macrophages (F4/80+ CD11b+), Th1 cells (CD69+ CD4+), and Th2 cells (CD69+ CD8+) so on.

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Others

Other Targets

TGF-beta/Smad

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2348795-14-0

364.438

C22H24N2O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (274.39 mM; Ultrasonic )

O=C(C=CC1=CC=C(OC)C=C1)NC2=CC=CC(=C2)C(=O)NC3CCCC3

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(-20℃)

With Ice Pack

≥ 2 years