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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C23H25N5O
- Peso molecular:387.48
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
TLR7 2.36 μM (Kd) |
TLR8 105 nM (Kd) |
TLR7 3.22 μM (IC50) |
TLR8 0.24 μM (IC50) |
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.
-
Cell Line:R848-stimulated THP-1 macrophages and PBMCs
-
Concentration:0.1, 1, 10, 20 μM
-
Incubation Time:6 h
-
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].
-
Cell Line:R848-stimulated THP-1 macrophages
-
Concentration:5, 10 μM
-
Incubation Time:0.5 h
-
Result:Downregulated the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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]
-
Dosage:0.5%, 1.0% ointment
-
Administration:topical, once daily, 7 days
-
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
-
Peso molecular 387.48
-
Fòrmula C23H25N5O
-
SMILES
OC1=CC=C(N2C=NC3=C2C4=CC=CC=C4N=C3N5CCN(CC)CC5)C=C1C
-
Envío
Room temperature in continental US; may vary elsewhere.
-
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)
SMU-R39 Related Classifications
HY-175782 Related Classifications
Powered by Bioz