NF-56-EJ40

Last updated

NF-56-EJ40
NF-56-EJ40 structure.png
Identifiers
  • 2-(2-(4'-((4-Methylpiperazin-1-yl)methyl)-[1,1'-biphenyl]-3-carboxamido)phenyl)acetic acid
CAS Number
PubChem CID
Chemical and physical data
Formula C27H29N3O3
Molar mass 443.547 g·mol−1
3D model (JSmol)
  • CN1CCN(CC1)CC2=CC=C(C=C2)C3=CC(=CC=C3)C(=O)NC4=CC=CC=C4CC(=O)O
  • InChI=1S/C27H29N3O3/c1-29-13-15-30(16-14-29)19-20-9-11-21(12-10-20)22-6-4-7-24(17-22)27(33)28-25-8-3-2-5-23(25)18-26(31)32/h2-12,17H,13-16,18-19H2,1H3,(H,28,33)(H,31,32)
  • Key:UTWXDNZWMQAUKL-UHFFFAOYSA-N

NF-56-EJ40 is an experimental drug which acts as a potent and selective antagonist for the succinate receptor SUCNR1 (GPR91). It has antiinflammatory effects and has been used to investigate the role of succinate in the development of conditions such as atherosclerosis and ulcerative colitis. [1] [2] [3] [4]

References

  1. Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, et al. (October 2019). "Structural basis of species-selective antagonist binding to the succinate receptor". Nature. 574 (7779): 581–585. Bibcode:2019Natur.574..581H. doi:10.1038/s41586-019-1663-8. PMID   31645725.
  2. Xu J, Zheng Y, Zhao Y, Zhang Y, Li H, Zhang A, et al. (2022). "Succinate/IL-1β Signaling Axis Promotes the Inflammatory Progression of Endothelial and Exacerbates Atherosclerosis". Frontiers in Immunology. 13: 817572. doi: 10.3389/fimmu.2022.817572 . PMC   8901997 . PMID   35273600.
  3. Shenol A, Lückmann M, Trauelsen M, Lambrughi M, Tiberti M, Papaleo E, et al. (March 2024). "Molecular dynamics-based identification of binding pathways and two distinct high-affinity sites for succinate in succinate receptor 1/GPR91". Molecular Cell. 84 (5): 955–966.e4. doi:10.1016/j.molcel.2024.01.011. PMID   38325379.
  4. Huo L, Chen Q, Jia S, Zhang Y, Wang L, Li X, et al. (August 2025). "Gut microbiome promotes succinate-induced ulcerative colitis by enhancing glycolysis through SUCNR1/NF-κB signaling pathway". American Journal of Physiology. Cell Physiology. 329 (2): C440 –C454. doi:10.1152/ajpcell.00411.2025. PMID   40549551.