J-1149
J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research.
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- No. CAS: 2883580-95-6
- Fòrmula: C25H24N8O
- Peso molecular:452.51
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Almacenamiento:
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Actividad biológica
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ALK5 0.017 μM (IC50) |
p38α MAPK |
J-1149 (compound 15g) (5-40 μM, 24 h) efficiently inhibits extracellular matrix (ECM) deposition in TGF-β-induced hepatic stellate cells (HSCs), and eventually suppresses HSC activation[1].
J-1149 (20 μM, 24 h) inhibits the expression of α-SMA and collagen I stimulated by TGF-β[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 cells
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Concentration:20 μM
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Incubation Time:1 h prior to TGF-β stimulation for continuous 24 h
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Result:Inhibited the expression of α-SMA and collagen I stimulated by TGF-β.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (SD) rats[1]
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Dosage:4 mg/kg (IV), 15 mg/kg (PO)
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Administration:IV or PO, once (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of J-1149 in male Sprague-Dawley rats[1].
IV (4 mg/kg) PO (15 mg/kg) Tmax (h) 0.00 ± 0.00 0.11 ± 0.13 Cmax (ng/mL) 43,144 ± 35,001 1386 ± 882 AUC0-t (ng/mL∗h) 12,529 ± 978 1217 ± 20 AUC0-∞ (ng/mL∗h) 12,802 ± 1160 2667 ± 1136 t1/2 (h) 2.24 ± 1.05 9.14 ± 5.13 CL (mL/h/kg) 314 ± 28 6564 ± 3372 F (%) 2.59%