MAC-545496
Based on 1 Customer Validation
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 838810-96-1
- Formula: C18H18ClN5O3S
- Molecular Weight:419.89
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Glycopeptide-resistance-associated protein R (GraR)[1]
MAC-545496 potently synergizes with Cefuroxime; concentrations as low as 0.03 µg/mL (~75 nM) lowers the β-lactam MIC from 512 to 8 µg/mL against S. aureus USA300. MAC545496 also synergizes with Cefuroxime and Oxacillin against a collection of ten S. aureus clinical isolates. In addition, MAC-545496 potentiates the effect of Cefuroxime against representatives of other circulating MRSA strains such as USA100, USA400 and USA500 to different extents, with the exception of CMRSA4, a USA200/EMRSA16 isolate. MAC-545496 also synergizes with the antimicrobial peptides colistin and polymyxin B[1].
MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the IC50 value is 0.0376 µg/mL[1].
MAC-545496 also inhibits the citrateinduced biofilm formation in the wild type in a concentration dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 838810-96-1
-
Appearance Solid
-
Molecular Weight 419.89
-
Formula C18H18ClN5O3S
-
Color Light yellow to yellow
-
SMILES
O=C(NC(NC1=NC=C(Cl)C=C1)=S)C2=CC=C(N3CCCCC3)C([N+]([O-])=O)=C2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 250 mg/mL (595.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3816 mL | 11.9079 mL | 23.8158 mL | 59.5394 mL |
| 5 mM | 0.4763 mL | 2.3816 mL | 4.7632 mL | 11.9079 mL | |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3816 mL | 5.9539 mL | |
| 15 mM | 0.1588 mL | 0.7939 mL | 1.5877 mL | 3.9693 mL | |
| 20 mM | 0.1191 mL | 0.5954 mL | 1.1908 mL | 2.9770 mL | |
| 25 mM | 0.0953 mL | 0.4763 mL | 0.9526 mL | 2.3816 mL | |
| 30 mM | 0.0794 mL | 0.3969 mL | 0.7939 mL | 1.9846 mL | |
| 40 mM | 0.0595 mL | 0.2977 mL | 0.5954 mL | 1.4885 mL | |
| 50 mM | 0.0476 mL | 0.2382 mL | 0.4763 mL | 1.1908 mL | |
| 60 mM | 0.0397 mL | 0.1985 mL | 0.3969 mL | 0.9923 mL | |
| 80 mM | 0.0298 mL | 0.1488 mL | 0.2977 mL | 0.7442 mL | |
| 100 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.5954 mL |