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 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.

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ETI60

ETI60 Chemical Structure

CAS No. : 2773475-11-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

ETI60 Related Antibodies

Top Publications Citing Use of Products

View All Toll-like Receptor (TLR) Isoform Specific Products:

View All Isoforms
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

View All p38 MAPK Isoform Specific Products:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

View All TNF Receptor Isoform Specific Products:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All ERK Isoform Specific Products:

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ERK ERK1 ERK2 ERK5 ERK8

View All JNK Isoform Specific Products:

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JNK1 JNK2 JNK3 JNK

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All Interleukin Related Isoform Specific Products:

View All Isoforms
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 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

In Vitro

ETI60 (0-200 μM, 4-24 h) effectively inhibits TLR agonist (e.g., Imiquimod (IMQ) (HY-B0180) for TLR7, ODN2395 (HY-150743) for TLR9)-induced TNF-α production in mouse macrophages (RAW 264.7) and human B lymphoblasts (Daudi) cell lines in a dose-dependent manner, without inducing cytotoxic effects[1].
ETI60 (24 h) inhibits TLR3, TLR7, and TLR9 with IC50 values ranging from 20 to 300 nM, and TLR8 with an IC50 of approximately 2 μM, and inhibits TLR3, TLR7 and TLR8 in a concentration-dependent manner (from 31.2 nM to 10 μM)[1].
ETI60 (5-10 μM, 20 min-8 h) 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[1].
ETI60 (10 μM, 2-4 h) attenuates the IMQ-induced upregulation of multiple inflammation-related genes, including IL1-β, CXCL2, IL18RAP, TNF, PDCD1, NLRP3, NFKBIZ, CCL3, CCL4, KDM6B, ZC3H12A, and PTGS2[1].

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

ETI60 Related Antibodies

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.
In Vivo

ETI60 (60 mg/kg, p.o., daily from day 2 to day 5) ameliorates psoriasis induced by IMQ in mice[1].
ETI60 (60 mg/kg, p.o., daily from day 2 to day 9) ameliorates psoriasis induced by IL-23 in mice[1].
ETI60 (30 mg/kg, p.o., daily for 39 days) effectively ameliorates symptoms in a mouse model of SLE[1].

MedChemExpress (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.
Molecular Weight

352.47

Formula

C21H28N4O
CAS No.
Appearance

Solid

SMILES

NC1=C(C(C=CC(OC)=C2)=C2N3CCCN(C)C)C3=NC4=C1CCCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (283.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8371 mL 14.1856 mL 28.3712 mL
5 mM 0.5674 mL 2.8371 mL 5.6742 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8371 mL 14.1856 mL 28.3712 mL 70.9280 mL
5 mM 0.5674 mL 2.8371 mL 5.6742 mL 14.1856 mL
10 mM 0.2837 mL 1.4186 mL 2.8371 mL 7.0928 mL
15 mM 0.1891 mL 0.9457 mL 1.8914 mL 4.7285 mL
20 mM 0.1419 mL 0.7093 mL 1.4186 mL 3.5464 mL
25 mM 0.1135 mL 0.5674 mL 1.1348 mL 2.8371 mL
30 mM 0.0946 mL 0.4729 mL 0.9457 mL 2.3643 mL
40 mM 0.0709 mL 0.3546 mL 0.7093 mL 1.7732 mL
50 mM 0.0567 mL 0.2837 mL 0.5674 mL 1.4186 mL
60 mM 0.0473 mL 0.2364 mL 0.4729 mL 1.1821 mL
80 mM 0.0355 mL 0.1773 mL 0.3546 mL 0.8866 mL
100 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7093 mL
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ETI60 Related Classifications

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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