MAC-545496
MAC-545496 is potent GraR inhibitor (glycopeptide-resistance-associated protein R). MAC-545496 reverses β-lactam resistance in the community-acquired MRSA USA300 strain. MAC-545496 could also serve as an antivirulence agent alone; it attenuates MRSA virulence in Galleria mellonella larvae. MAC-545496 inhibits biofilm formation and abrogates intracellular survival in macrophages. Mechanistic characterization revealed MAC-545496 to be a nanomolar inhibitor of GraR, a regulator that responds to cell-envelope stress and is an important virulence factor and determinant of antibiotic resistance. MAC-545496 has value as a research tool to probe the GraXRS regulatory system and as an antibacterial lead series of a mechanism to combat drug-resistant Staphylococcal infections.
For research use only. We do not sell to patients.
Chemical Information
| Name | MAC-545496 |
|---|---|
| Iupac Chemical Name | N-((5-chloropyridin-2-yl)carbamothioyl)-3-nitro-4-(piperidin-1-yl)benzamide |
| Synonyms | MAC-545496; MAC 545496; MAC545496; |
| Molecular Formula | C18H18ClN5O3S |
| Molecular Weight | 419.884 |
| Smile | O=C(NC(NC1=NC=C(Cl)C=C1)=S)C2=CC=C(N3CCCCC3)C([N+]([O-])=O)=C2 |
| InChiKey | AFOKREIUUQFDNW-UHFFFAOYSA-N |
| InChi | InChI=1S/C18H18ClN5O3S/c19-13-5-7-16(20-11-13)21-18(28)22-17(25)12-4-6-14(15(10-12)24(26)27)23-8-2-1-3-9-23/h4-7,10-11H,1-3,8-9H2,(H2,20,21,22,25,28) |
| CAS Number | 838810-96-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
El-Halfawy OM, Czarny TL, Flannagan RS, et al. Discovery of an antivirulence compound that reverses β-lactam resistance in MRSA. Nat Chem Biol. 2020;16(2):143–149. doi:10.1038/s41589-019-0401-8
Chemical Structure
