TGF-β1/Smad3-IN-2
TGF-β1/Smad3-IN-2 is an orally active antifibrotic agent. TGF-β1/Smad3-IN-2 has high affinity for VDR and can inhibit the TGFβ/SMAD3 signaling pathway. TGF-β1/Smad3-IN-2 inhibits hepatic stellate cell activation, reduces extracellular matrix deposition, and alleviates liver fibrosis in a bile duct ligation mouse model. TGF-β1/Smad3-IN-2 can be used for the research of liver fibrosis.
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- Fòrmula: C38H47NO3
- Peso molecular:565.78
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
TGF-β1/Smad3-IN-2 (compound D13) (0.1 μM; 24 h) significantly downregulates the Collagen I (COL1A1) and α-SMA (ACTA2) markers in TGF-β1-induced human LX-2 hepatic stellate cells (HSCs)[1].
TGF-β1/Smad3-IN-2 exhibits extremely low cytotoxicity in human hepatic stellate cell line LX-2, with an IC50 > 50 μM[1].
TGF-β1/Smad3-IN-2 (0.1 μM; 48 h) induces 654 downregulated differentially expressed genes and 507 upregulated DEGs in TGF-β1-stimulated human hepatic stellate cell line LX-2, among which core fibrotic genes (COL1A1, COL1A2, COL3A1) are significantly downregulated, with significant enrichment in the TGF-β signaling pathway, ECM-receptor interaction pathway and Hippo signaling pathway[1].
TGF-β1/Smad3-IN-2 promotes the direct interaction between VDR and SMAD3 proteins in human hepatic stellate cell line LX-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LX-2 human hepatic stellate cells (HSCs)
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Reduced α-SMA and collagen I protein levels to near baseline.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 8 weeks old, liver fibrosis induced by common bile duct ligation)[1]
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Dosage:100 μg/kg
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Administration:oral gavage; once daily; 2 weeks
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Result:Markedly ameliorated hepatic inflammation and reduced collagen accumulation in liver tissue, with efficacy comparable to calcipotriol.
Significantly downregulated hepatic expression of pro-fibrotic genes Ctgf, Fn, and Timp-1.
Significantly reduced serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bile acids (TBA).
Did not induce significant changes in serum calcium levels.
Chemical Information
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Peso molecular 565.78
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Fòrmula C38H47NO3
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SMILES
O=C(N(CC1=CC=CC=C1)CC2=CC=CC=C2)/C=C/[C@H]([C@H]3CC[C@H]([C@]3(C)CCC/4)C4=C\C=C(C[C@@H](O)C[C@@H]5O)/C5=C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TGF-β1/Smad3-IN-2 Related Classifications
HY-182038 Related Classifications
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