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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Toll-like Receptor (TLR)-ETI60
ETI60

Chemical Structure : ETI60

CAS No.: 2773475-11-7

ETI60 (endosomal TLR inhibitor 60)

货号: PC-25491Not For Human Use, Lab Use Only.

ETI60 (endosomal TLR inhibitor 60) is a potent, selective inhibitor of endosomal Toll-like receptors (TLR3, TLR7, TLR8 and TLR9) with IC50 of 20-3 00 nM for TLR3, TLR7 and TLR9, and 2 uM for TLR8.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ETI60 (endosomal TLR inhibitor 60) is a potent, selective inhibitor of endosomal Toll-like receptors (TLR3, TLR7, TLR8 and TLR9) with IC50 of 20-3 00 nM for TLR3, TLR7 and TLR9, and 2 uM for TLR8.
ETI60 effectively suppresses the secretion of pro-inflammatory cytokines mediated by endosomal TLR3, TLR7, TLR8 and TLR9 in various cell types, including RAW 264.7 macrophages, human Daudi cells and THP-1 monocytes, as well as in primary murine BMDCs.
ETI60 does not inhibits any plasma membrane TLR, including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5, in differentiated human THP-1 cells activated by FSL-1, Pam3CSK4, LPS and FLA-ST, respectively.
ETI60 (10 uM) inhibits IMQ- or ODN2395-induced phosphorylation of MAPKs (p-ERK, p-JNK and p-p38), nuclear translocation of the NF-κB p65 subunit, Iκ-Bα degradation and IRF7 expression in RAW 264.7 cells.
ETI60 ameliorated IMQ-induced autoimmune diseases by suppressing the expression of inflammation-associated genes.
ETI60 (60 mg/kg, daily, oral) ameliorate IMQ- and IL-23-induced psoriasis in mice.
ETI60 (30 mpk) in the MRL/lpr female mouse model of SLE. 

物理化学性质&存储条件

分子量 352.48
分子式 C21H28N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(3-(dimethylamino)propyl)-8-methoxy-2,3,4,6-tetrahydro-1H-indolo[2,3-b]quinolin-11-amine

参考文献

1. Jeong U, et al. Exp Mol Med. 2025 Sep 1. doi: 10.1038/s12276-025-01526-w.

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