| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
With an IC50 of 2.4 μg/mL, M62812 (10 μg/mL; 6 h) totally blocks LPS-induced NF-κB activation in NF-κB luciferase-expressing cells[1]. With an IC50 of 0.7 μg/mL, M62812 (3 μg/mL; 6 h) totally suppresses TNF-α production in peripheral blood mononuclear cells stimulated by LPS[1]. In human endothelial cells, M62812 (3 μg/mL; 6 h) totally suppresses the production of IL-6 and E-selection, with IC50 values of 0.43 μg/mL and 1.4 μg/mL, respectively [1].
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| ln Vivo |
M62812 (iv; 10–20 mg/kg; single dose) protects against endotoxic shock in a D-galactosamine-sensitized mice model by lowering coagulation and inflammatory markers[1]. By using the mouse cecal ligation and puncture paradigm, M62812 (iv; 20 mg/kg; once daily for three days) avoids mouse death[1].
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| Animal Protocol |
Animal/Disease Models: D-galactosamine-sensitized endotoxin shock mouse model[1]
Doses: 10-20 mg/kg Route of Administration: intravenous (iv) administration (iv) Experimental Results: 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/Disease Models: Cecal ligation and puncture mouse model[1] Doses: 20 mg/kg Route of Administration: intravenous (iv) administration ( iv); one time/day for three days Experimental Results: decreased mortality in a murine cecal ligation and puncture model. |
| References |
[1]. Nakamura M, et al. Toll-like receptor 4 signal transduction inhibitor, M62812, suppresses endothelial cell and leukocyte activation and prevents lethal septic shock in mice. Eur J Pharmacol. 2007 Aug 27;569(3):237-43.
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| Molecular Formula |
C13H13CL2N3OS
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|---|---|
| Molecular Weight |
330.23
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| CAS # |
613263-00-6
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| Related CAS # |
M62812 free base;613262-61-6
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| SMILES |
Cl.Cl.NC1C=CC=CC=1OC1C=CC2C(N)=NSC=2C=1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
0.1 M HCL: ≥ 50 mg/mL (151.41 mM)
DMSO: 50 mg/mL (151.41 mM) H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (7.57 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3028 mL | 1.5141 mL | 3.0282 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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