Home Microbiology Anti-infection inhibitor MAC-545496

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MAC-545496 Anti-infection inhibitor

Cat.No.S6771

MAC-545496 is a nanomolar glycopeptide-resistance-associated protein R(GraR) inhibitor with strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). This compound can reverse β-lactam resistance in methicillin-resistant strains and synergize with CAMPs. It shows remarkable activity in macrophages and attenuates S. aureus virulence in a G. mellonella larvae infection model.
MAC-545496 Anti-infection inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 419.89

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Quality Control

Batch: S677101 DMSO]84 mg/mL]false]Water]˂1 mg/mL]false]Ethanol]˂1 mg/mL]false Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (200.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 419.89 Formula

C18H18ClN5O3S

 

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 838810-96-1 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CCN(CC1)C2=C(C=C(C=C2)C(=O)NC(=S)NC3=NC=C(C=C3)Cl)[N+](=O)[O-]

Mechanism of Action

Targets/IC50/Ki
GraR
(Cell-free assay)
0.1 nM(Kd)
In vitro

MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the half-maximal inhibitory concentration (IC50) is 0.0376 µg/mL—matching with the concentration range of the synergistic effect with cefuroxime. This compound only inhibits the citrate-induced biofilm formation in the wild type in a concentration-dependent manner, suggesting additional potential as a lead for drug discovery. Treatment of S. aureus-infected macrophages with different doses of this chemical added 30 min after phagocytosis shows that it halts S. aureus replication within macrophages starting at 0.5 µg/mL..
In vivo

MAC-545496 activity is evidenced by increased survival of the drug-treated larvae as compared to infected untreated ones. This corresponds to concentration-dependent killing of S. aureus in the hemolymph of the larvae observed from the CFUs recovered from the hemolymph 200 min after infection. This matchs with the attenuated virulence of the graR::Tn mutant relative to the wild type in Galleria. Treatment with this compound recapitulates the phenotype of ΔgraR and ΔgraS mutants, effectively inhibiting intracellular S. aureus growth..
References

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