1. Neuronal Signaling Anti-infection
  2. Glucosylceramide Synthase (GCS) Bacterial
  3. G43

G43 是一种有效的选择性 glucosyltransferase 抑制剂,对 GtfB 和 GtfC 的Kd 值分别为3.7 μM和46.9 nM。G43 在体内外具有抗变形链球菌 (S. mutans) 的作用,可用于龋齿研究。

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G43 Chemical Structure

G43 Chemical Structure

CAS No. : 690693-02-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

体外研究
(In Vitro)

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%[1]
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% [1]
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[1]。 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[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: S. mutans. UA159 cells
Concentration: 3.125, 6.25, 12, 25 μM
Incubation Time: 24 h
Result: Showed no significant difference on expression of gtfs (gtfB, gtfC and gtfD).
体内研究
(In Vivo)

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[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The rat model of dental caries infected with S. mutans UA159[1]
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.
分子量

341.34

Formula

C16H11N3O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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