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.

For research use only. We do not sell to patients.

ETI60

ETI60 Chemical Structure

CAS No. : 2773475-11-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

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:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All TNF Receptor Isoform Specific Products:

View All Isoforms
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

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All JNK Isoform Specific Products:

View All Isoforms
JNK1 JNK2 JNK3 JNK

View All NF-κB Isoform Specific Products:

View All Isoforms
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

  • 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.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

ETI60 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ETI60
Cat. No.:
HY-178169
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.