| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
TLR2 (Toll-like receptor 2), specifically TLR2/1 and TLR2/6 heterodimers.
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| ln Vitro |
MMG-11 does not exhibit cytotoxicity or disrupt signaling that is triggered by TLR agonists, IL-1β, or TNF. Peripheral blood mononuclear cells (PBMC) exhibit up to 100 cell cytotoxicity assay in response to MMG-11 (0.01-100 µM) [1].
MMG-11 is a potent and selective TLR2 antagonist that inhibits TLR2/1 and TLR2/6 signaling. It inhibits Pam3CSK4-induced hTLR2/1 with an IC50 of 1.7 µM and Pam2CSK4-induced hTLR2/6 responses with an IC50 of 5.7 µM. The compound preferentially inhibits TLR2/1 over TLR2/6 heterodimer-mediated signaling in both human and murine species, with pA2 values of 5.73 and 6.15 for TLR2/1. It inhibits NF-κB/AP-1 activation with an IC50 of 0.87 µM. MMG-11 is a pyrogallol derivative identified by structure-based virtual screening. |
| ln Vivo |
In vivo efficacy data for MMG-11 is limited. The compound is primarily used as an in vitro tool for studying TLR2 biology and its role in innate immunity and inflammation. As a TLR2 antagonist, it has potential applications in treating inflammatory diseases where TLR2 signaling is dysregulated. Further in vivo studies in animal models of inflammation would be needed to assess its therapeutic potential.
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| Enzyme Assay |
The in vitro receptor binding assay for TLR2 antagonism uses cells expressing human TLR2/1 or TLR2/6 heterodimers along with the NF-κB-luciferase reporter system. Cells are treated with MMG-11 at varying concentrations (typically 0.01 to 100 µM) for 30-60 minutes, then stimulated with the TLR2/1 ligand Pam3CSK4 or the TLR2/6 ligand Pam2CSK4. After 4-6 hours of stimulation, luciferase activity is measured. The IC50 for inhibition of NF-κB/AP-1 activation is calculated from dose-response curves. Selectivity is assessed by profiling against other TLRs.
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: PBMC Tested Concentrations: 0.01, 1, 10, 100 µM Incubation Duration: Experimental Results: Up to 100 µM shows no cytotoxic effects [1]. In vitro cellular assays are performed using human embryonic kidney (HEK) cells expressing TLR2/1 or TLR2/6 heterodimers with an NF-κB-luciferase reporter, or using human peripheral blood mononuclear cells (PBMCs). Cells are pre-incubated with MMG-11 at concentrations ranging from 0.01 to 100 µM for 30-60 minutes, then stimulated with Pam3CSK4 (TLR2/1) or Pam2CSK4 (TLR2/6). NF-κB activation is measured by luciferase activity (for reporter cell lines) or by measuring cytokine production (e.g., IL-6, TNF-α) by ELISA (for PBMCs). Cytotoxicity is assessed using MTT or LDH release assays. |
| Animal Protocol |
In vivo animal model data for MMG-11 is not extensively reported in the literature. As a research tool for studying TLR2 biology in inflammation, the compound would typically be evaluated in mouse models of TLR2-mediated inflammation, such as LPS-induced sepsis or other inflammatory disease models. Standard efficacy studies would involve compound administration (oral or intraperitoneal) followed by assessment of inflammatory cytokine levels, immune cell infiltration, and tissue pathology. Pharmacokinetic studies would assess oral bioavailability, plasma half-life, and tissue distribution.
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| ADME/Pharmacokinetics |
MMG-11 has a molecular weight of 306.27 g/mol and molecular formula C15H14O7. It has a purity of 97% by HPLC. The compound is a pyrogallol derivative. It is soluble in DMSO and should be stored as a powder at -20°C. Pharmacokinetic parameters such as oral bioavailability, plasma half-life, and tissue distribution are not extensively characterized in publicly available literature. As a research compound, it is typically used in in vitro assays at concentrations ranging from nanomolar to low micromolar.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for MMG-11. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for TLR2 antagonists would typically include selectivity profiling against a panel of TLRs to assess off-target effects, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential. The compound is supplied as a solid and should be stored desiccated at -20°C.
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| References | |
| Additional Infomation |
MMG-11 is a research-grade TLR2 antagonist that inhibits TLR2/1 and TLR2/6 signaling. It is not approved for clinical use. The compound is a pyrogallol derivative identified by structure-based virtual screening. MMG-11 preferentially inhibits TLR2/1 over TLR2/6 heterodimer-mediated signaling in both human and murine species. It inhibits NF-κB/AP-1 activation with an IC50 of 0.87 µM. MMG-11 is supplied as a solid with high purity and should be stored desiccated at -20°C.
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| Molecular Formula |
C15H14O7
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|---|---|
| Molecular Weight |
306.267465114594
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| Exact Mass |
306.074
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| CAS # |
313254-94-3
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| Related CAS # |
MMG-11 quarterhydrate
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| PubChem CID |
854609
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| Appearance |
Light yellow to brown solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
411
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C(=O)OCC)=CC=C1CC(C1C=CC(=C(C=1O)O)O)=O
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| InChi Key |
IIDUJWIVMGALOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14O7/c1-2-21-15(20)12-6-3-8(22-12)7-11(17)9-4-5-10(16)14(19)13(9)18/h3-6,16,18-19H,2,7H2,1H3
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| Chemical Name |
ethyl 5-[2-oxo-2-(2,3,4-trihydroxyphenyl)ethyl]furan-2-carboxylate
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| Synonyms |
MMG-11 MMG 11 MMG11
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~100 mg/mL (~326.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 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 20.8 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: ≥ 2.08 mg/mL (6.79 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2651 mL | 16.3255 mL | 32.6509 mL | |
| 5 mM | 0.6530 mL | 3.2651 mL | 6.5302 mL | |
| 10 mM | 0.3265 mL | 1.6325 mL | 3.2651 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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