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MMG-11 quarterhydrate

Cat. No. M14129
MMG-11 quarterhydrate Structure
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Biological Activity

MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.

Chemical Information
Molecular Weight 310.78
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Marcel Bermudez, et al. Biological Characterization, Mechanistic Investigation and Structure-Activity Relationships of Chemically Stable TLR2 Antagonists

[2] Maria Grabowski, et al. The novel small-molecule antagonist MMG-11 preferentially inhibits TLR2/1 signaling

[3] Maria Grabowski, et al. Identification of a pyrogallol derivative as a potent and selective human TLR2 antagonist by structure-based virtual screening

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