2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. M62812

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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M62812 Chemical Structure

M62812 Chemical Structure

CAS No. : 613263-00-6

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Based on 1 publication(s) in Google Scholar

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M62812 Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

M62812 (i.v.; 10-20 mg/kg; single dose) is protective and reduces inflammatory and coagulation parameters in a D-galactosamine-sensitized endotoxin shock mouse model[1].
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.

Animal Model: D-galactosamine-sensitized endotoxin shock mouse model[1]
Dosage: 10-20 mg/kg
Administration: Intravenous administration (i.v.)
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.
Animal Model: Cecal ligation and puncture mouse model[1]
Dosage: 20 mg/kg
Administration: Intravenous administration (i.v.); once a day for three days
Result: Reduced mortality in a murine cecal ligation and puncture model.
Molecular Weight

330.23

Formula

C13H13Cl2N3OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NSC2=C1C=CC(OC3=CC=CC=C3N)=C2.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0282 mL 15.1410 mL 30.2819 mL
5 mM 0.6056 mL 3.0282 mL 6.0564 mL
View the 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  Saline

    Solubility: 2.5 mg/mL (7.57 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

* 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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M62812 Related Classifications

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:

M62812613263-00-6M 62812M-62812Toll-like Receptor (TLR)toll-like receptors (TLRs)TLR4LipopolysaccharidesepsisInhibitorinhibitorinhibit

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