TJN-331
TJN-331 is a potent and orally active TGF-β1 Inhibitor. TJN-331 ameliorates anti-glomerular basement membrane (GBM) nephritis in rats by inhibitng TGF-β1 production, thereby reducing extracapillary proliferation in glomeruli. TJN-331 inhibits mesangial expansion in experimental IgA nephropathy in ddY mice. TJN-331 can be used for the research of nephritis and IgA nephropathy.
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- CAS No.: 219964-53-1
- Formule: C19H22N2O3
- Masse moléculaire:326.39
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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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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
In Vitro
TJN-331 (1-50 μmol/L; 24-48 h) dose-dependently inhibits total and mature TGF-β1 production and reverses the decrease in Smad 2 and Smad 3 mRNA expression, and inhibits plasminogen mRNA expression in isolated glomeruli from anti-GBM nephritic rats[1].
TJN-331 (10-100 μmol/L; 48 hours) dose-dependently inhibits TGF-β1 production from splenocytes stimulated with ConA[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TJN-331 (0.1, 0.5, and 2.0 mg/kg; p.o.;daily for 5 weeks from week 10 to week 15) improves renal function and histopathological changes in glomeruli in an IgA nephropathy model in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SD rats injected with goat γ-globulin and goat anti-rat GBM serum[1]
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Dosage:0.1, 0.5, and 2.0 mg/kg
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Administration:p.o.; daily for 21 days from day 21 to day 41
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Result:Prevented urinary protein excretion at 2 mg/kg from day 30 to day 41, and showed significant inhibition only at day 35 at 0.5 mg/kg. showed a tendency to inhibit nephritis induced increase in serum creatinine levels. Inhibited crescent formation and adhesion in the anti-GBM nephritic glomeruli at 2 mg/kg. Inhibited the increase of a-Smooth Muscle Actin (SMA) and TGF-β1-positive areas. Inhibited the increase in glomerular production of mature at 2 mg/kg.
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Animal Model:Male ddY mice (7-week-old) induced by oral administration of bovine γ-globulin, followed by reticuloendothelial blocking by colloidal carbon injection and heminephrectomy.[2]
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Dosage:0.1, 0.5, and 2.0 mg/kg
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Administration:p.o.; daily for 5 weeks (from week 10 to week 15 after induction)
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Result:Inhibited increases in the mesangial matrix index and the number of nuclei per glomerular cross-section. Prevented increase in glomerular TGF-β1 staining without affecting IgA deposition. Did not influence urine volume during the experiments.
Chemical Information
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CAS No. 219964-53-1
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Masse moléculaire 326.39
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Formule C19H22N2O3
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SMILES
O=C(/C=C/C1=CN=CC=C1)N(C)CCC2=CC(OC)=C(C=C2)OC
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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
[1]. Saegusa Y, et al. TJN-331 improves anti-glomerular basement membrane nephritis by inhibiting the production of intraglomerular transforming growth factor-beta1. Biol Pharm Bull. 2010;33(8):1349-1354. [Content Brief]
[2]. Saegusa Y, et al. (E)-N-[(3,4-dimethoxyphenethyl)]-N-methyl-3-(3-pyridyl)-2-propenamide (TJN-331) inhibits mesangial expansion in experimental IgA nephropathy in ddY mice. Clin Exp Nephrol. 2010 Dec;14(6):528-35. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TJN-331 Related Classifications
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