CU-115

CAS: 2471982-20-2 货号: C655192 分子式: C21H11F7INO2 分子量: 569.21 PubChem CID: 154734323
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
C655192-1ml
期货 Stock Image
¥5,280.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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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.

IC50& Target:TLR8 1.04 μM (IC 50 ) TLR7 50 μM (IC 50 )

规格

规格或纯度
10mM in DMSO
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
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
小分子
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

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