SMU-L11-R
SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies.
For research use only. We do not sell to patients.
- CAS No.: 3040320-18-8
- Formula: C19H24N4O
- Molecular Weight:324.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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human TLR7 0.024 μM (EC50) |
TLR8 2.56 μM (EC50) |
SMU-L11-R (0-100 μM; 24 h; HEK-Blue hTLR7 cells) shows no obvious toxic effect[1].
SMU-L11-R (0-100 μM; 24 h; MC38 and B16-F10 cells) shows cytotoxic in MC38 and B16-F10 cells at a high testing concentration (100 μM)[1].
SMU-L11-R (0, 0.1, 1, 5, 10 μM; 24 h; Peritoneal macrophages) shows dose-dependent increase in M1-like macrophages[1][1].
SMU-L11-R (1 μM; 15-120 min; BMDCs) can activate TLR7 downstream signaling pathways through MyD88 protein, including the NF-κB, MAPK signaling pathways[1].
SMU-L11-R (0, 0.01, 0.1, 1, 10 μM; 24 h; HEK-Blue hTLR7 cells) shows dose-dependent increase in TLR7 protein[1].
SMU-L11-R (0-10 μM; 24 h; Raw 264.7 cells) shows significant increase in TNF-α and IL-6[1].
SMU-L11-R (0-10 μM; 24 h; human PBMCs) shows dose-dependent increase in TNF-α and IL-1β[1].
SMU-L11-R (0-10 μM; 24 h; mouse BMDCs) shows significant increase in IL-6[1].
SMU-L11-R (0, 0.1, 1, 10 μM; 24 h; peritoneal macrophages) shows concentration-dependent increase in NO production[1].
SMU-L11-R also shows the activation of TLR8 (EC50 = 2.56 μM) with the increase of concentration, but the activation was 156 times smaller than that of TLR7. SMU-L11-R induces activation of HEK-Blue hTLR2, hTLR3 or hTLR4 was negligible[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-Blue hTLR7 cells
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Concentration:0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM
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Incubation Time:24 h
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Result:Showed no obvious toxic effect.
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Cell Line:MC38 cells
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Concentration:0.02 μM, 0.05 μM, 0.14 μM, 1.23 μM, 11.11 μM, 33.33 μM, 100 μM
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Incubation Time:24 h
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Result:Showed cytotoxic effect at a high testing concentration (100 μM).
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Cell Line:B16-F10 cells
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Concentration:0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM
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Incubation Time:24 h
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Result:Showed cytotoxic effect at a high testing concentration (100 μM).
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Cell Line:HEK-Blue hTLR7 cells
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Concentration:0, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Showed dose-dependent increase in TLR7 protein.
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Cell Line:BMDCs
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Concentration:1 μM
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Incubation Time:15 min, 30 min, 60 min, 90 min, 120 min
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Result:Showed significant induction of the phosphorylation of IKK α/ β, p65, p38 and ERK1/2 in BMDCs.
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Cell Line:Raw 264.7 cells
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Concentration:0, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Showed significant increase in TNF-α and IL-6.
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Cell Line:Mouse BMDCs
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Concentration:0, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Showed significant increase in IL-6.
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Cell Line:Human PBMCs
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Concentration:0, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Showed dose-dependent increase in TNF-α and IL-1β.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/BL6 wild-type male mice (6-8 weeks old) were injected subcutaneousely with 2 x 105 MC38 cells[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:IP; every 2 days; 15 days
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Result:Significantly inhibited tumor growth and exhibited excellent synergistic anti-tumor effects when combined with PD-L1 inhibitors by upregulating CD8+ T cells.
Chemical Information
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CAS No. 3040320-18-8
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Molecular Weight 324.42
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Formula C19H24N4O
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SMILES
NC1=NC2=CC=CC=C2C3=C1N=C(CCCC)N3C[C@@H]4COCC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)