ETI60
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.51%
- CAS No.: 2773475-11-7
- Formule: C21H28N4O
- Masse moléculaire:352.47
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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TLR7 0.68 μM (IC50) |
TLR9 0.12 μM (IC50) |
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.
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Cell Line:murine RAW 264.7 and human Daudi cells
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Concentration:1.6-200 μM
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Incubation Time:24 h
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Result:Exhibited no cytotoxicity in both murine RAW 264.7 and human Daudi cells at concentrations up to 10 μM.
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Cell Line:RAW 264.7 cells
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Concentration:5 and 10 μM
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Incubation Time:20, 30, 40, and 50 min, 6 and 8 h
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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.
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.
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Animal Model:Female MRL/MpJ-Faslpr/J lupus-prone mice (14 weeks old)[1]
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Dosage:30 mg/kg
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Administration:p.o., daily for 39 days
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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.
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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]
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Dosage:60 mg/kg
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Administration:p.o., daily from day 2 to day 5
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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.
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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]
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Dosage:60 mg/kg
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Administration:p.o., daily from day 2 to day 9
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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.
Chemical Information
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CAS No. 2773475-11-7
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Appearance Solid
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Masse moléculaire 352.47
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Formule C21H28N4O
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Color Light brown to gray
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SMILES
NC1=C(C(C=CC(OC)=C2)=C2N3CCCN(C)C)C3=NC4=C1CCCC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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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