MAC13243 HClCAS号： 1071638-38-4分子式： C20H25Cl2N3O2S分子量： 442.4描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)
| 产品描述 | |
| 描述 |
MAC13243 HCl, an inhibitor of LolA, a periplasmic chaperone that transports lipoproteins from the inner membrane to the outer membrane, is an antimicrobial agent with specificity and significant inhibitory effects on Gram-negative bacteria.
|
| 纯度 |
98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 可溶性/溶解性 |
DMSO:50 mg/mL (113.02 mM)
|
| 生物活性 | |
| In vitro(体外研究) |
We investigated the impact of a prototype drug (MAC13243 HCl) interfering with the Gram-negative outer membrane protein LolA on the faecal microbiota. Faecal suspensions from two healthy human donors were exposed to MAC13243 HCl (16, 32, or 64 mg/L) using an in vitro gut model (CoMiniGut). Samples collected 0, 4, and 8 h after exposure were subjected to viable cell counts, 16S rRNA gene quantification and V3-V4 sequencing using the Illumina MiSeq platform. MAC13243 HCl exhibited concentration-dependent killing of coliforms in both donors after 8 h. Concentrations of ≤32 mg/L reduced the growth of aerobic bacteria without influencing the microbiota composition and diversity. An expansion of Firmicutes at the expense of Bacteroidetes and Actinobacteria was observed in the faecal microbiota from one donor following exposure to 64 mg/L of MAC13243 HCl. At all concentrations tested, MAC13243 HCl did not lead to the proliferation of Escherichia coli nor a reduced abundance of beneficial bacteria, which are typical changes observed in antibiotic-induced dysbiosis. These results support our hypothesis that a drug interfering with a specific target in Gram-negative bacteria has a low impact on the commensal gut microbiota and, therefore, a low risk of inducing dysbiosis.[3]
|