[CAS NO. 838810-96-1] MAC-545496
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PRODUCTS SPECIFICATIONS [838810-96-1]
Catalog
SLK-S6771
Brand
Selleck
CAS
838810-96-1
DESCRIPTION [838810-96-1]
Overview
| MDL | MFCD05848166 |
|---|---|
| Molecular Weight | 419.89 |
| Molecular Formula | C18H18ClN5O3S |
| SMILES | O=C(NC(NC1=NC=C(Cl)C=C1)=S)C2=CC=C(N3CCCCC3)C([N ]([O-])=O)=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3816 mL | 11.9079 mL | 23.8158 mL |
| 5 mM | 0.4763 mL | 2.3816 mL | 4.7632 mL |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3816 mL |
| 50 mM | 0.0476 mL | 0.2382 mL | 0.4763 mL |
Description
MAC-545496 is a nanomolar inhibitor with strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 can reverse β-lactam resistance in methicillin-resistant strains and synergize with CAMPs. MAC-545496 shows remarkable activity in macrophages and attenuates S. aureus virulence in a G. mellonella larvae infection model.
Targets
| GraR [1] (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. MAC-545496 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 MAC-545496 added 30 min after phagocytosis shows that the MAC-545496 halts S. aureus replication within macrophages starting at 0.5 µg/mL..
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