MD2-TLR4-IN-1
Based on 1 publication(s) in Google Scholar
MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex antagonist. MD2-TLR4-IN-1 inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced expression of TNF-α and IL-6 in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. MD2-TLR4-IN-1 can be used for the study of acute lung injury (ALI).
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- Pureza: 98.16%
- No. CAS: 2249801-12-3
- Fòrmula: C22H14Cl2N4O
- Peso molecular:421.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MD2-TLR4-IN-1
More
Actividad biológica
Descripciòn
IC50 & Target
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TLR4 |
In Vitro
MD2-TLR4-IN-1 (compound 22m) exerts its anti-inflammatory activity by inhibiting NF-κB in RAW264.7 macrophages[1].
MD2-TLR4-IN-1 is directly bound to the MD2-TLR4 complex and disrupted MD2-TLR4 activation[1].
MD2-TLR4-IN-1 suppresses the NF-κB p65 subunit nuclear levels in LPS-induced macrophages[1].
MD2-TLR4-IN-1 binds to recombinant MD2 and TLR4 proteins with Kd values of 185 and 146 μM, respectively, while it does not interact with the intracellular adaptor protein MyD88[1].
MD2-TLR4-IN-1 significantly inhibits dimerization of the MD2-TLR4
complex in LPS-activated mouse primary macrophages (MPMs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (18-22 g) injectied intraperitoneally with LPS (20 mg/kg)[1].
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Dosage:5 mg/kg, 10 mg/kg
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Administration:Tail vein injection; once; 15 min before LPS injection
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Result:Effectively reduced airspace inflammation and amended the tissue structure of pulmonary lobules.
Significantly decreases LPS-induced myeloperoxidase (MPO) activity. Reduced LPS-induced serum TNF-α levels.
Decreased the mRNA levels of TNF-α, IL-6, IL-1β, IL-12, and IL-33 in lung tissues. In addition, COX-2 mRNA levels were also reduced.
Chemical Information
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No. CAS 2249801-12-3
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Appearance Solid
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Peso molecular 421.28
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Fòrmula C22H14Cl2N4O
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Color White to off-white
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SMILES
ClC1=C(C(NC2=CC(C(C3=CC=C(NC=C4)C4=C3)=NN5)=C5C=C2)=O)C(Cl)=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 83.33 mg/mL (197.80 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3737 mL | 11.8686 mL | 23.7372 mL | 59.3430 mL |
| 5 mM | 0.4747 mL | 2.3737 mL | 4.7474 mL | 11.8686 mL | |
| 10 mM | 0.2374 mL | 1.1869 mL | 2.3737 mL | 5.9343 mL | |
| 15 mM | 0.1582 mL | 0.7912 mL | 1.5825 mL | 3.9562 mL | |
| 20 mM | 0.1187 mL | 0.5934 mL | 1.1869 mL | 2.9671 mL | |
| 25 mM | 0.0949 mL | 0.4747 mL | 0.9495 mL | 2.3737 mL | |
| 30 mM | 0.0791 mL | 0.3956 mL | 0.7912 mL | 1.9781 mL | |
| 40 mM | 0.0593 mL | 0.2967 mL | 0.5934 mL | 1.4836 mL | |
| 50 mM | 0.0475 mL | 0.2374 mL | 0.4747 mL | 1.1869 mL | |
| 60 mM | 0.0396 mL | 0.1978 mL | 0.3956 mL | 0.9890 mL | |
| 80 mM | 0.0297 mL | 0.1484 mL | 0.2967 mL | 0.7418 mL | |
| 100 mM | 0.0237 mL | 0.1187 mL | 0.2374 mL | 0.5934 mL |
MD2-TLR4-IN-1 Related Classifications
HY-128598 Related Classifications
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