1821387-73-8
1821387-73-8 結構式
基本信息
N-methyl-4-nitro-2-[4-[4-(trifluoromethyl)phenyl]imidazol-1-yl]aniline
Benzenamine, N-methyl-4-nitro-2-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-
物理化學性質(zhì)
常見問題列表
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TLR2 52.9 nM (EC 50 , in HEK-Blue cells) |
TLR1 52.9 nM (EC 50 , in HEK-Blue cells) |
CU-T12-9 directly targets TLR1/2 to initiate downstream signaling. By binding to both TLR1 and TLR2, CU-T12-9 facilitates the TLR1/2 heterodimeric complex formation, which in turn activates the downstream signaling.
CU-T12-9 activates the TLR1/2 pathway by inducing NF-κB activation to trigger downstream signaling, such as secreted embryonic alkaline phosphatase (SEAP), NO, and TNF-α.
CU-T12-9 (0.39-100 μM; 24 hours) does not produce toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells.
CU-T12-9 up-regulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) activates TLR1 mRNA and iNOS mRNA after Raw 264.7 cells are treated for 24 hours. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after Raw 264.7 cells are treated for 2 hours. CU-T12-9 (0.1-10 μM) activates TNF mRNA after Raw 264.7 cells are treated for 8 hours.
Cell Cytotoxicity Assay
| Cell Line: | HEK-Blue hTLR2 and Raw 264.7 macrophage cells |
| Concentration: | 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50, and 100 μM |
| Incubation Time: | 24 hours |
| Result: | No toxicity was seen up to 100 μM. |
RT-PCR
| Cell Line: | Raw 264.7 cells |
| Concentration: | 0.1, 1, 10 μM |
| Incubation Time: |
24 hours for TLR1 and iNOS mRNA assay
2 hours for TLR2 and IL-10 mRNA assay 8 hours for TNF mRNA assay |
| Result: |
Triggered TLR1 mRNA and iNOS mRNA at 24 hours dose-dependently.
Dose-dependent activation of TLR2 mRNA and IL-10 mRNA at 2 hours. Showed dose-dependent activation of TNF mRNA at 8 hours. |