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CU-115

CAS No. 2471982-20-2

CU-115 ( N-(4-(3,5-bis(trifluoromethyl)phenoxy)phenyl)-2-fluoro-6-iodobenzamide )

产品货号. M28821 CAS No. 2471982-20-2

CU-115 是 TLR8 的选择性拮抗剂,对 TLR8 和 TLR7 的 IC50 分别为 1.04 μM 和 >50 μM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥1416 有现货
10MG ¥2261 有现货
25MG ¥3841 有现货
50MG ¥5375 有现货
100MG ¥7137 有现货
500MG ¥14490 有现货
1G 获取报价 有现货
1 mL x 10 mM in DMSO ¥1767 有现货

生物学信息

  • 产品名称
    CU-115
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    CU-115 是 TLR8 的选择性拮抗剂,对 TLR8 和 TLR7 的 IC50 分别为 1.04 μM 和 >50 μM。
  • 产品描述
    CU-115 is a selective antagonist of TLR8 with IC50s of 1.04 μM and >50 μM for TLR8 and TLR7, respectively.(In Vitro):CU-115 (1, 5, and 20 μM) inhibits TLR9 to 10-25% inhibition. CU-115 (5-20 μM) inhibits increases in the activity of type I IFN transcriptional induced by the ssRNA nucleic acid ligands 3p-hpRNA or G3-YSD. CU-115 (5-20 μM) abolishes the TNF-α production activated by R848 (1 μg/ml) and represses the expression of IL-1β in hTHP-1 cells. CU-115 does not modulate the NF-kB inhibition induced by Pam2CSK4, Pam3CSK4, LPS, R848, Poly(I:C), and Flic in HEK-293 TLR1/2, TLR2/6, TLR3, and TLR4 cells.
  • 体外实验
    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.
  • 体内实验
    ——
  • 同义词
    N-(4-(3,5-bis(trifluoromethyl)phenoxy)phenyl)-2-fluoro-6-iodobenzamide
  • 通路
    Immunology/Inflammation
  • 靶点
    TLR
  • 受体
    ABHD6
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    2471982-20-2
  • 分子量
    569.21
  • 分子式
    C21H11F7INO2
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO : 100 mg/mL (175.68 mM)
  • SMILES
    O=C(NC1=CC=C(OC=2C=C(C=C(C2)C(F)(F)F)C(F)(F)F)C=C1)C=3C(F)=CC=CC3I
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.Daniel A Bachovchin, et al. Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening. Proc Natl Acad Sci U S A. 2010 Dec 7;107(49):20941-6.
产品手册
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