2. Immunology/Inflammation MAPK/ERK Pathway Apoptosis Stem Cell/Wnt NF-κB
  3. Toll-like Receptor (TLR) p38 MAPK TNF Receptor ERK JNK NF-κB Interleukin Related
  4. ETI60

ETI60 是一种口服有效的选择性 TLR 抑制剂，其靶向 TLR7 (IC50 = 0.68 μM) 和 TLR9 (IC50 = 0.12 μM) 的核苷结合位点 I 发挥作用，不影响表面 TLR (包括 TLR1/TLR2、TLR2/TLR6、TLR4 和 TLR5)。ETI60 在细胞、生物物理和体内实验中均表现出纳摩尔级别的活性，能有效抑制内体 TLR 介导的促炎信号。ETI60 可调节炎症相关基因的表达。ETI60 能有效改善银屑病和系统性红斑狼疮 (SLE) 小鼠模型的症状。ETI60 可用于自身免疫性疾病和炎症性疾病的相关研究。

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ETI60

ETI60 Chemical Structure

CAS No. : 2773475-11-7

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ETI60 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

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JNK1 JNK2 JNK3 JNK

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research[1].

IC50 & Target[1]

TLR7

0.68 μM (IC50)

TLR9

0.12 μM (IC50)

体外研究
(In Vitro)

ETI60 (0-200 μM，4-24 小时) 可有效抑制 TLR 激动剂 (例如，用于 TLR7 的 Imiquimod (IMQ, HY-B0180)，用于 TLR9 的 ODN2395 (HY-150743)) 诱导的小鼠巨噬细胞 (RAW 264.7) 和人 B 淋巴母细胞 (Daudi) 细胞系中 TNF-α 的产生，且呈剂量依赖性，并在此过程中不诱导细胞毒性效应[1]。
ETI60 (24 小时) 可抑制 TLR3、TLR7 和 TLR9，IC50 值在 20 至 300 nM 之间，抑制 TLR8 的 IC50 约为 2 μM，并在 31.2 nM 至 10 μM 的浓度范围内，以浓度依赖性方式抑制 TLR3、TLR7 和 TLR8 的活性[1]。
ETI60 (5-10 μM，20 分钟-8 小时) 在 RAW 264.7 细胞中，可抑制 IMQ 或 ODN2395 诱导的 MAPKs 磷酸化 (p-ERK、p-JNK 和 p-p38)、NF-κB p65 亚基的核转位、Iκ-Bα 降解以及 IRF7 的表达[1]。
ETI60 (10 μM，2-4 小时) 可减弱 IMQ 诱导的多个炎症相关基因的上调，包括 IL1-β、CXCL2、IL18RAP、TNF、PDCD1、NLRP3、NFKBIZ、CCL3、CCL4、KDM6B、ZC3H12A和PTGS2[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ETI60 相关抗体:

Cell Viability Assay[1]

Cell Line: murine RAW 264.7 and human Daudi cells
Concentration: 1.6-200 μM
Incubation Time: 24 h
Result: Exhibited no cytotoxicity in both murine RAW 264.7 and human Daudi cells at concentrations up to 10 μM.

Western Blot Analysis[1]

Cell Line: RAW 264.7 cells
Concentration: 5 and 10 μM
Incubation Time: 20, 30, 40, and 50 min, 6 and 8 h
Result: Reduced p-ERK, p-JNK and p-p38 levels.
Suppressed the nuclear translocation of the NF-κB p65 subunit.
Downregulated IRF7 expression and prevented the degradation of Iκ-Bα.
体内研究
(In Vivo)

ETI60 (60 mg/kg，口服，每日一次，从第 2 天到第 5 天) 可改善 IMQ 诱发的小鼠银屑病[1]。
ETI60 (60 mg/kg，口服，每日一次，从第 2 天到第 9 天) 可改善 IL-23 诱发的小鼠银屑病[1]。
ETI60 (30 mg/kg，口服，每日一次，持续 39 天) 能有效改善系统性红斑狼疮 (SLE) 小鼠模型中的症状[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female MRL/MpJ-Faslpr/J lupus-prone mice (14 weeks old)[1]
Dosage: 30 mg/kg
Administration: p.o., daily for 39 days
Result: Prevented weight gain or loss and decreased lymphnode weights.
Reduced alopecia and skin rashes compared with the vehicle and HCQ (60 mg/kg, P.O., daily for 39 days).
Increased complement C3 levels, indicating reduced disease activity and restored immune function.
Reduced serological markers associated with SLE, such as antinuclear antibody (ANA), anti-dsDNA antibodies and IgG in the kidney, compared to HCQ group.
Demonstrated significant reduction in SLE symptoms at half the dose of HCQ, suggesting high efficacy.
Animal Model: Female C57BL/6J mice (6 weeks old) induced with psoriasis via daily topical application of Aldara cream (IMQ, 62.5 mg/cm²) for 4 days post-shaving[1]
Dosage: 60 mg/kg
Administration: p.o., daily from day 2 to day 5
Result: Significantly reduced the Psoriasis Area and Severity Index (PASI) scores, epidermal acanthosis, dermal thickness and keratinocyte proliferation.
Inhibited IL-17A and IL-23 expression and dermal inflammatory cell infiltration.
Animal Model: Female C57BL/6J mice (6 weeks old) induced with psoriasis via intradermal injection of recombinant murine IL-23 (500 ng) around the ear daily for 8 days[1]
Dosage: 60 mg/kg
Administration: p.o., daily from day 2 to day 9
Result: Improved disease symptoms comparable to or superior to the positive control (anti-IL-17A antibody, 30 mg/kg, i.p., dose on day 2, 5, and 8), without significant differences in body weight.
Significantly decreased ear and epidermal thicknesses, CD68 expression and Ki-67 keratinocyte proliferation.
分子量

352.47

Formula

C21H28N4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ETI60 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ETI602773475-11-7ETI 60ETI-60Toll-like Receptor (TLR)p38 MAPKTNF ReceptorERKJNKNF-κBInterleukin RelatedTumor Necrosis Factor ReceptorTNFRExtracellular signal regulated kinasesc-Jun N-terminal kinaseNuclear factor-κBNuclear factor-kappaBILendosomal TLRsTCR9TCR7pro-inflammatory signalingpsoriasisSLEautoimmuneinflammatoryRAW 264.7DaudiTNF-αMAPKInhibitorinhibitorinhibit

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