LT-1339-553
LT-1339-553 is a selective, orally active RIPK1 inhibitor with IC50 values of 4.32, 95.74 and 84.33 nM against RIPK1, RIPK2 and RIPK3, respectively. LT-1339-553 exerts anti-necroptotic activity by inhibiting the AKT/PI3K/NF-κB pathway and the IL-17 pathway. LT-1339-553 reduces liver injury, inflammatory responses and collagen deposition. LT-1339-553 can be used in studies related to schistosomiasis-induced liver fibrosis.
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- No. CAS: 3078683-57-2
- Fòrmula: C21H13F5N4O3
- Peso molecular:464.34
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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RIPK1 4.32 nM (IC50) |
RIPK2 95.74 nM (IC50) |
RIPK3 84.33 nM (IC50) |
IL-17 |
LT-1339-553 potently protects human HT29 cells from necroptosis induced by TNFα/Smac-mimetic/z-VAD-FMK (HY-16658B) (TSZ), with an EC50 of 14.43 nM; meanwhile, this compound exhibits cytotoxicity at high concentrations, with an IC50 of 1760 nM[1].
LT-1339-553 potently protects mouse L929 cells from TSZ-induced necroptosis with an EC50 of 5.33 nM, and inhibits the phosphorylation of mouse RIPK1 in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LT-1339-553 (50-100 mg/kg; p.o.; daily; 4 weeks) significantly alleviates schistosomiasis-induced hepatic fibrosis in C57BL/6 mice, with the 100 mg/kg dose suppressing pro-inflammatory and profibrotic signaling pathways including AKT/PI3K/NF-κB and IL-17[1].
LT-1339-553 (400 mg/kg; p.o.; single dose) exhibits a favorable safety profile in ICR mice with no observed toxicity or organ damage over 14 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (infected percutaneously with S. japonicum cercariae, treated with praziquantel at 5 weeks postinfection to clear parasites)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 4 weeks
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Result:Significantly improved body weight recovery at weeks 8 and 9 postinfection compared to infected controls.
Reduced liver index from 8.67% to 6.14% and spleen index from 1.60% to 0.76% at 10 mg/kg.
Reduced serum ALT and AST levels, hepatic egg granuloma area, collagen deposition, liver hydroxyproline content, and liver ROS levels compared to infected controls, with significant effects at 10 mg/kg.
Decreased hepatic protein levels of Collagen I and α-SMA, with the 10 mg/kg dose showing more pronounced reduction.
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Animal Model:C57BL/6 (infected percutaneously with S. japonicum cercariae, treated with praziquantel at 5 weeks postinfection to clear parasites)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 4 weeks
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Result:Significantly improved body weight recovery at weeks 8 and 9 postinfection compared to infected controls.
Reduced liver index, spleen index, serum ALT and AST levels, hepatic egg granuloma area, collagen deposition, liver hydroxyproline content, and liver ROS levels compared to infected controls, with significant effects at both doses.
Decreased hepatic protein levels of Collagen I and α-SMA, with the 100 mg/kg dose showing more pronounced reduction.
Downregulated hepatic expression of inflammatory factors (TNF-α, IL-17, IL-1β) and chemokines (CXCL5/9/10/16, CCL2/4/5/7/11/22), and suppressed activation of the AKT/PI3K/NF-κB signaling pathway and necroptosis-related proteins (RIPK1, RIPK3, MLKL, and their phosphorylated forms) at 100 mg/kg.
Chemical Information
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No. CAS 3078683-57-2
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Peso molecular 464.34
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Fòrmula C21H13F5N4O3
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SMILES
NC1=NOC2=C1C(C3=C(C(F)=C(C=C3)NC(NC4=CC(OC(F)(F)F)=CC=C4)=O)F)=CC=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LT-1339-553 Related Classifications
HY-184001 Related Classifications
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