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.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | MAC-545496 |
|---|---|
| Iupac 化学名称 | N-((5-chloropyridin-2-yl)carbamothioyl)-3-nitro-4-(piperidin-1-yl)benzamide |
| 同义词 | MAC-545496; MAC 545496; MAC545496; |
| 英文同义词 | MAC-545496; MAC 545496; MAC545496; |
| 分子式 | C18H18ClN5O3S |
| 分子量 | 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号 | 838810-96-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| 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
