SMU-14a
SMU-14a is a selective Toll-like receptor 3 (TLR3) inhibitor wirh an IC50 of 0.18 μM. SMU-14a reduces phosphorylation of p65, ERK, and TBK1 via NF-κB, MAPK, and IRF3 signaling pathways. SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages, downregulates TNF-α in human peripheral blood monocytes and decreases serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used for the research of acute hepatitis.
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- Formule: C24H20N4O
- Masse moléculaire:380.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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TLR3 0.18 μM (IC50) |
TBK1 |
IL-6 |
p65 |
SMU-14a (1-10 μM; 24 h) potently inhibits TLR3 activity in HEK-Blue hTLR3 cells induced by Poly I:C (HY-107202) with an IC50 of 0.18 ± 0.02 μM and does not affect TLR2, TLR4, or TLR7 activity[1].
SMU-14a (0.01-1 μM; 24 h) dose-dependently reduces Poly I:C-induced IL-6 secretion in RAW 264.7 cells[1].
SMU-14a (0.01-1 μM; 24 h) dose-dependently reduces Poly I:C-induced TNF-α secretion in human peripheral blood mononuclear cells[1].
SMU-14a (0.01-1 μM; 24 h) does not induce cytotoxicity in human peripheral blood mononuclear cells after 24 h of incubation[1].
SMU-14a (0.01-1 μM; 4 h) dose-dependently inhibits Poly I:C-induced phosphorylation of p65, ERK, and TBK1 through the NF-κB, MAPK, and IRF3 signaling pathways in RAW 264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 cells
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Concentration:0.01, 0.1, 1 μM
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Incubation Time:4 h
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Result:Dose-dependently reversed Poly I:C-induced phosphorylation of p65 (NF-κB pathway), ERK (MAPK pathway), and TBK1 (IRF3 pathway) in RAW 264.7 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 6-8 weeks old, 20-22 g, tail vein injection of 20 mg/kg Concanavalin A)[1]
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Dosage:50 mg/kg
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Administration:single dose (0.5 hours before Concanavalin A challenge)
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Result:Significantly reduced serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and the inflammatory cytokine IL-6 compared to the untreated model group.
Reduced hepatic congestion, edema, and inflammatory cell infiltration, with preservation of liver lobule structure relative to the model group.
Chemical Information
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Masse moléculaire 380.44
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Formule C24H20N4O
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SMILES
O=C(C1=CC2=C(NC3=C2C(C)=C(C=NC=C4)C4=C3C)C=C1)NC5=CC=CC=C5N
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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)
SMU-14a Related Classifications
HY-176192 Related Classifications
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