Antifibrotic agent 4
Antifibrotic agent 4 is an antifibrotic agent. Antifibrotic agent 4 inhibits the expression of the fibrotic markers α-SMA and COL1A1 in hepatic stellate cells by binding to FGFR4 and reducing its autophosphorylation, ameliorates liver injury and collagen deposition in mouse models of liver fibrosis, and does not inhibit the hERG potassium channel. Antifibrotic agent 4 can be used in the research of liver fibrosis.
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- Formule: C29H35Br4N3O6
- Masse moléculaire:841.22
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LX-2 | IC50 |
12.612 μM
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Inhibition of viability of TGF-β-activated hepatic stellate LX2 cells incubated for 24 h by MTT cell viability assay.
Inhibition of viability of TGF-β-activated hepatic stellate LX2 cells incubated for 24 h by MTT cell viability assay.
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42593910 |
In Vitro
Antifibrotic agent 4 (compound C11) exhibits extremely weak inhibitory effect on the hERG potassium channel, with an IC50 value of > 100 μM, which eliminates the cardiotoxicity risk of the parent compound PD[1].
Antifibrotic agent 4 (10-20 μM; 24 h) inhibits the viability of activated LX2 cells, with an IC50 of 12.61 μM. It also reduces the expression of fibrosis markers and suppresses FGFR4 phosphorylation, retaining antifibrotic activity in vitro[1].
Antifibrotic agent 4 (1.5-400 μM) exhibits no toxicity to normal AML12 hepatocytes, and may promote the proliferation of these cells at concentrations of 13 μM and 25 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TGF-β-activated hepatic stellate LX2 cells
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Concentration:10, 20 μM
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Incubation Time:24 h
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Result:Inhibited viability of activated LX2 cells with an IC50 of 12.612 μM.
Dose-dependently reduced protein expression of fibrosis markers α-SMA and COL1A1.
Reduced autophosphorylation of FGFR4 (p-FGFR4) in activated LX2 cells.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | T1/2 | MRTINF_obs | Tmax | Cmax |
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| Rat[1] | 5 mg/kg | i.p. | 589 ng/mL·h | 592 ng/mL·h | 0.427 h | 0.87 h | 0.250 h | 904 ng/mL |
In Vivo
Antifibrotic agent 4 (10-50 mg/kg; i.p.; administered daily for 14 consecutive days) exhibits no observable in vivo toxicity in mice at doses up to 50 mg/kg with daily administration for 14 consecutive days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCl4-induced liver fibrosis in 6-week-old mice[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.p.; once daily; 2 weeks
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Result:Significantly improved liver index at 5 mg/kg and 10 mg/kg doses.
Reduced serum transaminase (ALT, AST) levels at 5 mg/kg and 10 mg/kg doses.
Attenuated hepatic inflammatory infiltration at 5 mg/kg and 10 mg/kg doses.
Reduced collagen deposition (confirmed via H&E, Masson, and Sirius Red staining) at 5 mg/kg and 10 mg/kg doses.
Exhibited inhibitory effect on hepatic α-SMA protein expression comparable to parent compound PD at 10 mg/kg.
Reduced hepatic Acta2 and Col1a1 mRNA levels at 10 mg/kg.
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Animal Model:acute toxicity testing[1]
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Dosage:10 mg/kg; 30 mg/kg; 50 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Caused no mortality at any tested dose.
Had no adverse effects on body weight, heart index, spleen index, lung index, or kidney index.
Maintained serum levels of CRE, BUN, AST, and ALT within normal ranges.
Showed no histopathological abnormalities in heart, liver, spleen, lung, or kidney tissues.
Chemical Information
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Masse moléculaire 841.22
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Formule C29H35Br4N3O6
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SMILES
BrC1=C(OCCCNC(C)=O)C(Br)=CC(C2C(C2)C(N(C)CCCOC3=C(Br)C=C(OCC(N(C)C)=O)C=C3Br)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antifibrotic agent 4 Related Classifications
HY-187994 Related Classifications
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Keywords
- Antifibrotic agent 4
- Antifibrotic agent4
- Antifibrotic agent-4
- Biochemical Assay Reagents
- CCl4-induced liver fibrosis
- COL1A1
- liver fibrosis mouse models
- Fibroblast Growth Factor Receptor 4
- AML12 normal hepatocytes
- α-SMA
- activated hepatic stellate cells
- hepatocytes
- LX2 cell
- hERG potassium channel
- Inhibitor
- inhibitor
- inhibit