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TGFβ1-IN-1 is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin). TGFβ1-IN-1 (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 IC50 of 105 μM.
TGFβ1-IN-1 (15 or 30 mg/kg, p.o., 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.
Molecular Weight | 364.44 |
Formula | C22H24N2O3 |
CAS Number | 2348795-14-0 |
Solubility (25°C) | DMSO 75 mg/mL |
Storage | 4°C, protect from light, dry, sealed |
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