|N3,N5,3'-三甲基-4'-(((2R,3S,4S,5S,6R)-3,4,5-三羟基-6-(羟甲基)四氢-2H-吡喃-2-基)氧基)-[1,1'-联苯]-3,5-二甲酰胺|CsnPharm

CAS No.: 1373346-85-0

M4284 Catalog No. CSN20333

Synonyms: M4284

M4284, a high-affinity inhibitory mannoside targeting FimH, reduces intestinal colonization of genetically diverse UPEC isolates, while simultaneously treating UTI, without notably disrupting the structural configuration of the gut microbiota.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述FimH is a mannose-binding adhesin located at the tip of the type 1 pilus produced by uropathogenic E. coli. M4284 is a biphenyl mannoside FimH antagonist. Its binding affinity for FimH is ~100,000-fold higher than D-mannose. In mice that were colonized with UTI89, a human cystitis isolate, in the gut and bladder, three oral doses of M4284 (100mg/kg) significantly reduced UTI89 levels in feces, cecum, and colon compared to the vehicle-treated controls. M4284 treatment also simultaneously reduced UTI89 levels in the gut and urinary tracts of mice. M4284 did not significantly change bacterial community structure in mice pretreated with streptomycin and then colonized with UTI89. In mice colonized with three additional genetically diverse UPEC clinical isolates (EC958, 41.4p, and CFT073), treatment with 100mg/kg M4284 reduced the levels of UPEC strain in the feces, cecum, and colon^[2].
参考文献

[1] Spaulding CN, Klein RD, et al. Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist. Nature. 2017 Jun 22;546(7659):528-532.
[2] Spaulding CN, Klein RD, Ruer S, Kau AL, Schreiber HL, Cusumano ZT, Dodson KW, Pinkner JS, Fremont DH, Janetka JW, Remaut H, Gordon JI, Hultgren SJ. Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist. Nature. 2017 Jun 22;546(7659):528-532.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1717 mL
- 10.8583 mL
- 21.7166 mL
- 5 mM
- 0.4343 mL
- 2.1717 mL
- 4.3433 mL
- 10 mM
- 0.2172 mL
- 1.0858 mL
- 2.1717 mL

技术信息

CAS号

1373346-85-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H28N2O8

运输

蓝冰

分子量

460.48

别名

M4284

溶解度

DMSO	120.0 mg/mL (260.6 mM) warming

动物实验配方

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