2. TGF-beta/Smad
  3. TGF-β Receptor
  4. 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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TJN-331

TJN-331 Chemical Structure

CAS No. : 219964-53-1

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Description

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[1][2].

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.

TJN-331 Related Antibodies
In Vivo

TJN-331 (0.1, 0.5, and 2.0 mg/kg; p.o.; once daily for 21 days from day 21 to day 41) reduces proteinuria and histopathological changes, and inhibits TGF-β1 protein production and positive areas in the anti-GBM induced nephritic rat model[1].
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.

Animal Model: Male SD rats injected with goat γ-globulin and goat anti-rat GBM serum[1]
Dosage: 0.1, 0.5, and 2.0 mg/kg
Administration: p.o.; daily for 21 days from day 21 to day 41
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.
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]
Dosage: 0.1, 0.5, and 2.0 mg/kg
Administration: p.o.; daily for 5 weeks (from week 10 to week 15 after induction)
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.
Molecular Weight

326.39

Formula

C19H22N2O3
CAS No.
SMILES

O=C(/C=C/C1=CN=CC=C1)N(C)CCC2=CC(OC)=C(C=C2)OC
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Room temperature in continental US; may vary elsewhere.
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References
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TJN-331 Related Classifications

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Keywords:

TJN-331219964-53-1TJN331TJN 331TGF-β ReceptorTransforming growth factor beta receptorsproteinuria,inhibition of TGF-beta1 production,anti-GBM nephritis,glomerulonephritis,TJN-331,glomeruli,Mesangium,histopathological changes,antinephritic effects,TGF-beta1 productionInhibitorinhibitorinhibit

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