TLR2 antagonist-1
TLR2 antagonist-1 is a selective Toll-like receptor 2 (TLR2) antagonist. TLR2 antagonist-1 can effectively inhibit excessive TLR2 activation (IC50 = 11.41 μM) and the production of inflammatory factors. TLR2 antagonist-1 has metabolic stability with a half-life (T1/2) of 16.67 min in mouse liver microsomes. TLR2 antagonist-1 can be used for the researches of inflammation, immunology, and neurological disease.
For research use only. We do not sell to patients.
- Formula: C18H15ClFN3O4
- Molecular Weight:391.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TLR2 11.41 μM (IC50) |
In Vitro
TLR2 antagonist-1 (Compound T30) exhibits low cytotoxicity with an CC50 value of 37.25 μM in RAW 264.7 cells[1].
TLR2 antagonist-1 (12.5-25 μM) inhibits hTLR2/NF-κB pathway in HEK-Blue hTLR2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 391.78
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Formula C18H15ClFN3O4
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SMILES
C/C(C1=CC=C(O)C(O)=C1Cl)=N\OCC2=CC(C3=NOC(C)=N3)=CC(F)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (255.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.38 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 (6.38 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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%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.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5525 mL | 12.7623 mL | 25.5245 mL | 63.8113 mL |
| 5 mM | 0.5105 mL | 2.5525 mL | 5.1049 mL | 12.7623 mL | |
| 10 mM | 0.2552 mL | 1.2762 mL | 2.5525 mL | 6.3811 mL | |
| 15 mM | 0.1702 mL | 0.8508 mL | 1.7016 mL | 4.2541 mL | |
| 20 mM | 0.1276 mL | 0.6381 mL | 1.2762 mL | 3.1906 mL | |
| 25 mM | 0.1021 mL | 0.5105 mL | 1.0210 mL | 2.5525 mL | |
| 30 mM | 0.0851 mL | 0.4254 mL | 0.8508 mL | 2.1270 mL | |
| 40 mM | 0.0638 mL | 0.3191 mL | 0.6381 mL | 1.5953 mL | |
| 50 mM | 0.0510 mL | 0.2552 mL | 0.5105 mL | 1.2762 mL | |
| 60 mM | 0.0425 mL | 0.2127 mL | 0.4254 mL | 1.0635 mL | |
| 80 mM | 0.0319 mL | 0.1595 mL | 0.3191 mL | 0.7976 mL | |
| 100 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6381 mL |
TLR2 antagonist-1 Related Classifications
HY-175533 Related Classifications
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