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编 号:F740969
分子式:C16H11N3O4S
分子量:341.34
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生物活性:
G43 is a potent, selective glucosyltransferase inhibitor, with the Kd of 3.7μM and 46.9 nM for GtfB and GtfC, respectively. G43 has antibacterial to S. mutans in vitro and in vivo, and can be used for dental caries study.

体内研究:
G43 (100?μM, 每天两次, 4 周, 局部给药) 可降低变形链球菌体内毒力。Animal Model:The rat model of dental caries infected with S. mutans UA159
Dosage:100?μM twice daily for 4 weeks
Administration:Topically administration
Result:Reduced the buccal, sulcal, and proximal surface caries scores, but did not lose weight over the course of the study.

体外研究:
G43 (16 h) 在12.5 μM浓度下对变形链球菌生物膜的抑制率达到 85%。G43 (25 μM, 24 h) 降低了糖基转移酶(glucosyltransferase, Gtfs) 的葡聚糖生成,并持续抑制 GtfB 和 GtfC 的活性,两种酶的抑制率均达 80% 。G43 (高达25 μM, 24 h) 对UA159 变异变性链球菌中 gtfs (gtfB, gtfC and gtfD) 的表达无显著影响。G43 (50 μM, 24-48 h) 通过减少野生型变形链球菌中水不溶性胞外多糖的产生来减少生物膜的形成。
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