MAC-545496 | MedChemExpress (MCE)

MAC-545496 产品活性：MAC-545496 是糖肽抗性相关蛋白 R (GraR) 的纳摩尔抑制剂。MAC-545496 对全长 GraR 蛋白具有很强的结合亲和力 (Kd ≤ 0.1 nM)。 MAC-545496 是一种抗毒剂，可逆转耐甲氧西林的菌株 (MRSA) 中的 β-内酰胺耐药性。 产品来源： https://www.medchemexpress.cn/mac-545496.html 研究领域：Anti-infection 作用靶点：Bacterial In Vitro: 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. MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the IC50 value is 0.0376 µg/mL. MAC-545496 also inhibits the citrateinduced biofilm formation in the wild type in a concentration dependent manner. In Vivo: In vivo, MAC-545496 is effective as a monotherapy for MRSA infected Galleria mellonella larvae. MAC-545496 activity is evidenced by increased survival of the drug-treated larvae as compared to infected untreated ones. This corresponded 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. Treatment of S. aureus-infected larvae with MAC-545496 occurred 30min after infection that mimics acquiring bacterial infection before initiating antimicrobial therapy . 相关产品：Bioactive Compound Library Plus | Anti-Infection Compound Library | Antibacterial Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Anti-Drug-Resistant Compound Library | Bioactive Compound Library Max | Rapamycin | Doxorubicin hydrochloride | Bafilomycin A1 | Dimethyl sulfoxide | Dexamethasone | Puromycin dihydrochloride | Staurosporine | Actinomycin D | Etoposide | G-418 disulfate | Nigericin sodium salt | 5-Azacytidine | Brefeldin A | CCCP | Estradiol | Ionomycin | Hygromycin B | Mitomycin C | Resveratrol | Tunicamycin | Everolimus | Doxycycline hyclate | Tacrolimus | Methotrexate | Streptozotocin | Lactate sodium | Neomycin sulfate | Acetaminophen | Anisomycin 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。

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