计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
CU-115 is a potent TLR8 antagonist ( IC 50 =1.04 µM ), and shows selective for TLR8 over TLR7 (IC 50 =>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:TLR8 1.04 μM (IC 50 ) TLR7 50 μM (IC 50 )
规格
规格或纯度
≥99%
英文名称
CU-115
生化机理
CU-115 是一种强效的 TLR8 拮抗剂（IC 50 =1.04 µM），对 TLR8 的选择性高于 TLR7（IC 50 =>50 µM）。CU-115 可减少 THP-1 细胞在 R-848 激活下产生的 TNF-α 和 IL-1β。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
拮抗剂
纯度
≥99%
名称和识别符
分子类型
未知
IUPAC Name
N-[4-[3,5-bis(trifluoromethyl)phenoxy]phenyl]-2-fluoro-6-iodobenzamide
INCHI
1S/C21H11F7INO2/c22-16-2-1-3-17(29)18(16)19(31)30-13-4-6-14(7-5-13)32-15-9-11(20(23,24)25)8-12(10-15)21(26,27)28/h1-10H,(H,30,31)
InChi Key
QYSLCRYVUJORPX-UHFFFAOYSA-N
Smiles
C1=CC(=C(C(=C1)I)C(=O)NC2=CC=C(C=C2)OC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)F
Isomeric SMILES
C1=CC(=C(C(=C1)I)C(=O)NC2=CC=C(C=C2)OC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)F
PubChem CID
分子量
569.21
技术文档
高级数据
三维结构
交互式化学结构模型
关联靶点（人）
THP-1
(11052 活性数据)
HEK293
(82097 活性数据)
关联靶点（其它种属）
RAW264.7 (28094 活性数据)
Tlr7
Toll-like receptor 7 (174 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 100 mg/mL (175.68 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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