M4284

Names

[ Name ]:
M4284

[Synonym ]:
5-[4-[(2{r},3{s},4{s},5{s},6{r})-6-(Hydroxymethyl)-3,4,5-Tris(Oxidanyl)oxan-2-Yl]oxy-3-Methyl-Phenyl]-{n}1,~{n}3-Dimethyl-Benzene-1,3-Dicarboxamide
4'-(α-D-Mannopyranosyloxy)-N,N',3'-trimethyl-3,5-biphenyldicarboxamide
[1,1'-Biphenyl]-3,5-dicarboxamide, 4'-(α-D-mannopyranosyloxy)-N3,N5,3'-trimethyl-

Biological Activity

[Description]:

M4284 (M-4284) is a high-affinity biphenyl mannoside FimH inhibitor with HAI of 16 nM in hemagglutination assay; reduces intestinal colonization of genetically diverse UPEC isolates, while simultaneously treating UTI, without notably disrupting the structural configuration of the gut microbiota; reduces UTI89 levels in the gut and urinary tracts of mice.

[Related Catalog]:

Research Areas >> Infection

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Anti-infection >> Bacterial

[Target]

IC50: FimH[1]

[In Vivo]

M4284 (oral administration; 100 mg/kg; 3 doses) can reduces UTI89 levels in the gut and urinary tracts of mice that are concurrently colonized with UTI89 in the gut and bladder. And treating mice with additonal M4284 doses further reduces the UTI89 population and the number of UPEC is lower in M4284-treated mice after termination of treatment[1]. Animal Model: C3H/HeN mice[1]. Dosage: 100 mg/kg Administration: Oral administation; a single dose. Result: Had activities against different UPEC strains in different host genetic backgrounds and gut microbial community contexts.

[References]

[1]. Schaeffer EM, et al.Selective Depletion of Uropathogenic E. coli from the Gut by a FimH Antagonist.SelectivJ Urol. 2018 Apr;199(4):874-875.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
733.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₈N₂O₈

[ Molecular Weight ]:
460.477

[ Flash Point ]:
397.5±32.9 °C

[ Exact Mass ]:
460.184570

[ LogP ]:
-0.89

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.618

[ Storage condition ]:
-20°C