M62812
Based on 1 Customer Validation
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis.
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- Purity: 99.75%
- CAS No.: 613263-00-6
- 화학식: C13H13Cl2N3OS
- 분자량:330.23
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
M62812 (10 μg/mL; 6 h) completely inhibits LPS-induced NF-κB activation in NF-κB luciferase-expressing cells with an IC50 of 2.4 μg/mL[1].
M62812 (3 μg/mL; 6 h) completely inhibits LPS-induced TNF-α production in peripheral blood mononuclear cells with an IC50 of 0.7 μg/mL[1].
M62812 (3 μg/mL; 6 h) completely inhibits the production of IL-6 and E-selection in human endothelial cells with IC50s of 0.43 μg/mL and 1.4 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
M62812 (i.v.; 20 mg/kg; once a day for three days) prevents mice from lethality in a murine cecal ligation and puncture model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:D-galactosamine-sensitized endotoxin shock mouse model[1]
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Dosage:10-20 mg/kg
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Administration:Intravenous administration (i.v.)
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Result:Prevented elevation of TNF-α, IL-6, soluble E-selectin, thrombin/antithrombin complexes and glutamic pyruvic transaminase activity at 20 mg/kg.
Prolonged survival in a d-galactosamine-sensitized endotoxin shock mouse model.
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Animal Model:Cecal ligation and puncture mouse model[1]
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Dosage:20 mg/kg
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Administration:Intravenous administration (i.v.); once a day for three days
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Result:Reduced mortality in a murine cecal ligation and puncture model.
Chemical Information
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CAS No. 613263-00-6
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Appearance Solid
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분자량 330.23
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화학식 C13H13Cl2N3OS
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Color White to off-white
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SMILES
NC1=NSC2=C1C=CC(OC3=CC=CC=C3N)=C2.[H]Cl.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 50 mg/mL (151.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : ≥ 50 mg/mL (151.41 mM)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (7.57 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 (7.57 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: Saline
Solubility: 2.5 mg/mL (7.57 mM); Clear solution; Need ultrasonic
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (274 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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Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 / 0.1 M HCl | 1 mM | 3.0282 mL | 15.1410 mL | 30.2819 mL | 75.7048 mL |
| 5 mM | 0.6056 mL | 3.0282 mL | 6.0564 mL | 15.1410 mL | |
| 10 mM | 0.3028 mL | 1.5141 mL | 3.0282 mL | 7.5705 mL | |
| 15 mM | 0.2019 mL | 1.0094 mL | 2.0188 mL | 5.0470 mL | |
| 20 mM | 0.1514 mL | 0.7570 mL | 1.5141 mL | 3.7852 mL | |
| 25 mM | 0.1211 mL | 0.6056 mL | 1.2113 mL | 3.0282 mL | |
| 30 mM | 0.1009 mL | 0.5047 mL | 1.0094 mL | 2.5235 mL | |
| 40 mM | 0.0757 mL | 0.3785 mL | 0.7570 mL | 1.8926 mL | |
| 50 mM | 0.0606 mL | 0.3028 mL | 0.6056 mL | 1.5141 mL | |
| 60 mM | 0.0505 mL | 0.2523 mL | 0.5047 mL | 1.2617 mL | |
| 80 mM | 0.0379 mL | 0.1893 mL | 0.3785 mL | 0.9463 mL | |
| 100 mM | 0.0303 mL | 0.1514 mL | 0.3028 mL | 0.7570 mL |
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