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Synonyms:
TLR7 antagonist-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | TLR7antagonist-1 (Compound 44#) is an orally bioavailable and selective TLR7 antagonist with an IC50 value of 0.3 nM for TLR7. It specifically binds to TLR7, inhibiting its activation and downregulating the c-Rel signaling pathway. TLR7antagonist-1 also reduces the mRNA levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α and alleviates psoriasiform lesions induced by Imiquimod. This compound is applicable for psoriasis-related research. |
| Targets & IC50 | TLR7:0.3 nM |
| In vitro | TLR7 antagonist-1 potently and selectively inhibits TLR7 in HEK-Blue-HTLR7 cells with an IC50 of 0.3 nM, while showing significantly weaker activity against TLR8 and TLR9. Additionally, TLR7 antagonist-1 (0.005-5 μM; 12 h) suppresses TLR7-mediated inflammatory cytokines in a concentration-dependent manner in RAW264.7 and HEK-Blue-HTLR7 cells. |
| In vivo | TLR7 antagonist-1 (15-45 mg/kg; oral) effectively alleviates psoriasis-like skin inflammation, systemic immune response, and associated liver and kidney function damage induced by Imiquimod in female BALB/C mice, with a dose-dependent decrease in inflammation markers and tissue damage levels. |
| Molecular Weight | 455.90 |
| Formula | C21H25ClF3N5O |
| Cas No. | 3104353-70-7 |
| Smiles | Cl.FC(F)(F)C=1C=C(C=NC1N2CCC(N)(C)CC2)C=3C=C(OC)C4=NC(=CN4C3)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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