SMU-R39
SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.
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- Formule: C23H25N5O
- Masse moléculaire:387.48
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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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Activité biologique
Description
IC50 & Target
[1]|
TLR7 2.36 μM (Kd) |
TLR8 105 nM (Kd) |
TLR7 3.22 μM (IC50) |
TLR8 0.24 μM (IC50) |
In Vitro
SMU-R39 (0.1-30 μM, 24 h) shows potent inhibitory activity against R848-induced SEAP signal in HEK-Blue hTLR8 cells (IC50 = 0.24 μM) and moderate inhibitory activity in HEK-Blue hTLR7 cells (IC50 = 3.22 μM)[1].
SMU-R39 (0.01-10 μM, 24 h) strongly blocks Resiquimod (R848) (HY-13740)-induced SEAP signal elevation in THP1-Dual cells with an IC50 of 0.18 μM, demonstrating its ability to inhibit NF-κB activation via TLR7/8 signaling[1].
SMU-R39 (0.046-100 μM, 24 h) dose-dependently inhibited R848-activated TLR7/8 activation in HEK-Blue hTLR7/8 and THP1-Dual cells
SMU-R39 (5-10 μM, 0.5 h) downregulates the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages, suppressing TLR7/8 downstream NF-κB and MAPK signaling pathways[1].
SMU-R39 (0.1-20 μM, 24 h) significantly reduces TNF-α secretion in R848-stimulated THP-1 macrophages, Raw 264.7 cells, and PBMCs in a concentration-dependent manner[1].
SMU-R39 (0.1-20 μM, 6 h) effectively decreases the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:R848-stimulated THP-1 macrophages and PBMCs
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Concentration:0.1, 1, 10, 20 μM
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Incubation Time:6 h
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Result:Decreased the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs[1].
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Cell Line:R848-stimulated THP-1 macrophages
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Concentration:5, 10 μM
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Incubation Time:0.5 h
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Result:Downregulated the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages [1].
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:IMQ-induced psoriasis mouse model: 5% Imiquimod (IMQ) ointment (62.5 mg) was topically applied to the hairless dorsal skin of 8-12-week-old female BALB/c mice once daily for 7 consecutive days[1]
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Dosage:0.5%, 1.0% ointment
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Administration:topical, once daily, 7 days
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Result:Achieved a psoriasis area and severity index (PASI) reduction.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Downregulated the gene expression of skin TNF-α, IFN-α , IL-17 , IL-22 , and IL-23 .
Achieved an epidermal thickness reduction.
Chemical Information
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Masse moléculaire 387.48
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Formule C23H25N5O
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SMILES
OC1=CC=C(N2C=NC3=C2C4=CC=CC=C4N=C3N5CCN(CC)CC5)C=C1C
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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-R39 Related Classifications
HY-175782 Related Classifications
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