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TLR7/8 Agonist - Thiazoquinoline compound
CL075 (3M002) is a thiazoloquinolone derivative that, alike the base analog R848 (Resiquimod), induces differential TLR7 and/or TLR8 responses in human and murine immune cells.
CL075 was originally described as a human TLR8 (hTLR8) agonist because it triggers a potent NF-κB activation in hTLR8 reporter cells when compared to hTLR7 reporter cells .
In human peripheral blood mononuclear cells (PBMCs), CL075 induces the production of TNF-α and IL-12, and to a lesser extent IFN-α. This cytokine profile is similar to the one induced by the hTLR8 agonist ssRNA40 . CL075 also induces the NF-κB-dependent production of IL-1α/β, IL-6, IL-8, MIP-1αβ, and MIP-3αβ pro-inflammatory cytokines . CL075 efficiently stimulates cytokine production from monocytes and myeloid dendritic cells (DCs) among human PBMCs . This compound has been used to optimize the ex vivo maturation of monocyte-derived DCs for developing DC-based anti-pathogen or anti-tumor vaccines .
Using our reporter cell lines HEK-Blue™ hTLR7, HEK-Blue™ hTLR8, HEK-Blue™ mTLR7, and HEK-Blue™ mTLR8, we established that CL075 is a TLR7/8 agonist. CL075 is ~10 times more potent for hLTR8 activation than for hTLR7. It also activates murine TLR7 (mTLR7), but not mTLR8.
Key features of CL075:
- Agonist of hTLR7 and hTLR8 with higher potency towards hTLR8.
- Agonist of mTLR7.
- Each lot of CL075 is highly pure (>95%) and functionally tested.
1. Gorden K.B. et al., 2005. Synthetic TLR agonists reveal functional differences between human TLR7 and TLR8. J. Immunol. 174(3):1259-68.
2. Spranger S. et al., 2010. Generation of Th1-polarizing dendritic cells using the TLR7/8 agonist CL075. J. Immunol. 185:738-747
Specificity: human TLR7/8 and mouse TLR7 agonist
CAS number: 256922-53-9
Molecular weight: 243.33 g/mol
Solubility: 1 mg/ml in water
- 0.1 - 5 μg/ml CL075 for human TLR8 and mouse TLR7 in cell culture assays
- 0.5 - 5 μg/ml CL075 for human TLR7 in cell culture assays
- Purity: ≥95% (UHPLC)
- The biological activity of CL075 has been verified using cellular assays.
- The absence of bacterial contamination has been confirmed using HEK-Blue™ hTLR2 cells (for lipoproteins) and HEK-Blue™ hTLR4 cells (for endotoxins).
CL075 is available in two quantities:
- 500 µg CL075
- 2 ml of sterile endotoxin-free water
- 5 mg CL075
- 10 ml of sterile endotoxin-free water
CL075 is provided as a pale yellow lyophilized powder and shipped at room temperature.
Store at -20°C.
Lyophilized product is stable 1 year at -20°C when properly stored.
Resuspended CL075 should be aliquoted and stored at -20°C.
Resuspended product is stable 6 months at -20°C.
Avoid repeated freeze-thaw cycles.Back to the top
Chemical structure of CL075:
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