TGF-β/Smad-IN-2
TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. TGF-β/Smad-IN-2 inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation and collagen deposition, with an IC50 value of 102 μM for collagen reduction in LL29 cells. TGF-β/Smad-IN-2 exerts its effects through modulation of the SMAD3/SMAD7 signaling pathway. TGF-β/Smad-IN-2 reduces lung index in pulmonary fibrosis mice. TGF-β/Smad-IN-2 can be used for the study of pulmonary fibrosis.
For research use only. We do not sell to patients.
- Formula: C17H20N2O2
- Molecular Weight:284.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
TGF-β/Smad-IN-2 (Compound 10b) (50-100 μM, 48 h) significantly downregulates mRNA expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, COLLAGEN3α1, TIMP1, VIMENTIN) and inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation in LL29 cells and DHLF cells[1].
TGF-β/Smad-IN-2 (50-100 μM, 48 h) reduces protein levels of α-SMA, COLLAGEN3α1, and p-COFILIN in DHLF cells and restores E-CADHERIN expression under TGF-β stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LL29 cells and DHLF cells
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Concentration:50,100 μM
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Incubation Time:48 h
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Result:Downregulated mRNA expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, COLLAGEN3α1, TIMP1, VIMENTIN).
| Species | Dose | Route | Tmax | T1/2 | MRT | Cmax | AUC0-t |
|---|---|---|---|---|---|---|---|
| Rat[1] | 30 mg/kg | p.o. | 0.35 h | 0.83 h | 1.28 h | 2451.41 ng/mL | 3732.02 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BLMN (2 mg/kg in normal saline) was intratracheally administered to 6-week-old male C57BL/6 mice to establish the pulmonary fibrosis model[1]
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Dosage:150, 300 mg/kg
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Administration:i.g., once daily, 14 days
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Result:Achieved lung index reduction.
Showed no significant changes in body weight and no abnormal hematological parameters (RBC, WBC, hemoglobin, platelets) or pathological changes.
Reduced the mRNA and protein expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, TIMP3) in lung tissues.
Appeared downregulation of phosphorylated Smad3 and upregulation of Smad7 in lung tissues.
Showed improvement in lung function (reduced respiratory resistance and elastance, increased quasi-static compliance).
Achieved reduction in collagen deposition in lung tissues.
Chemical Information
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Molecular Weight 284.35
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Formula C17H20N2O2
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SMILES
O=C1C(CN2CCOCC2)=CC(C)=CN1C3=CC=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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