化合物CU-115
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- CAS号:
- 2471982-20-2
- 英文名:
- Benzamide, N-[4-[3,5-bis(trifluoromethyl)phenoxy]phenyl]-2-fluoro-6-iodo-
- 英文别名:
- Benzamide, N-[4-[3,5-bis(trifluoromethyl)phenoxy]phenyl]-2-fluoro-6-iodo-
- 中文名:
- 化合物CU-115
- 中文别名:
- 化合物CU-115
- CBNumber:
- CB48376376
- 分子式:
- C21H11F7INO2
- 分子量:
- 569.21
- MOL File:
- 2471982-20-2.mol
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化合物CU-115化学性质
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沸点:
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427.3±45.0 °C(Predicted)
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密度:
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1.713±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMF: 10mg/mL,DMSO: 10mg/mL,DMSO:PBS (pH 7.2) (1:5): 0.15mg/mL,Ethanol: 0.25mg/mL
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形态:
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A crystalline solid
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酸度系数(pKa):
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11.28±0.70(Predicted)
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化合物CU-115性质、用途与生产工艺
CU-115 是一种强有力的 TLR8 拮抗剂 (IC50=1.04 µM),并显示了对 TLR8 选择性高于TLR7 (IC50=>50 µM)。CU-115 降低了由 R-848 激活的 THP-1 细胞 TNF-α 和 IL-1β 的产生。
TLR8
1.04 μM (IC
50
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TLR7
50 μM (IC
50
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In endosomal and non-endosomal TLR specificity studies, Human embryonic kidney (HEK) 293 cells expressing human tolllike receptor (hTLR) gene and an inducible secreted embryonic alkaline phosphatase (SEAP) reporter gene were incubated with CU-115 for 16 hours. As a result, CU-115 displays activity for TLR7 and TLR8 at low concentrations (0.5 μM).CU-115 does not modulate the NF-kB inhibition induced by Pam2CSK4, Pam3CSK4, Poly(I:C), LPS, R848, and Flic in HEK-293 TLR1/2, TLR2/6, TLR3, and TLR4 cells. And CU-115 inhibits TLR9 signaling at 1, 5, and 20 µM and ~10-25% inhibition.CU-115 (5-20 µM) inhibits increases in type I IFN transcriptional activity induced by the ssRNA nucleic acid ligands 3p-hpRNA or G3-YSD in a luciferase reporter assay.CU-115 (0.5, 1.0, 5, and 20 µM; 16 hours) is nontoxic at low concentrations (0.5 and 20 μM) and toxic at 100 μM in Hek293 TLR7 and TLR8 cells. CU-115 also is nontoxic at low concentrations (0.5 and 20 μM) and displays partial toxicity at 100 μM in THP Dual cells.The enzyme-linked immunosorbent assay (ELISA) is performed to measure upregulation/inhibition of TNF-α in human THP-1 cells (hTHP-1). CU-115 (5-20 µM) abolishes the TNF-α production activated by R848 (1 µg/ml) in hTHP1. It also represses the expression of IL-1β in hTHP-1 cells. These results suggest that CU-115 suppresses TLR8 and TLR7 signaling pathways.
化合物CU-115
上下游产品信息
上游原料
下游产品
2471982-20-2, 化合物CU-115 相关搜索:
- C21H11F7INO2
- 化合物CU-115
- 2471982-20-2
- Benzamide, N-[4-[3,5-bis(trifluoromethyl)phenoxy]phenyl]-2-fluoro-6-iodo-