TM5441

TM5441 is a drug which acts as an inhibitor of the serpin protein plasminogen activator inhibitor-1 (PAI-1). By inhibiting PAI-1, it increases activity of the enzymes tissue plasminogen activator and urokinase, which are involved in the blood clotting cascade. It has been researched for conditions such as hepatic steatosis and diabetic nephropathy, and while it has not been developed for medical use, it is widely used in scientific research.[1][2][3][4]

TM5441
Clinical data
ATC code
  • None
Identifiers
  • 5-chloro-2-(2-(2-((3-(furan-3-yl)phenyl)amino)-2-oxoethoxy)acetamido)benzoic acid
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC21H17ClN2O6
Molar mass428.83 g·mol−1
3D model (JSmol)
  • C1=CC(=CC(=C1)NC(=O)COCC(=O)NC2=C(C=C(C=C2)Cl)C(=O)O)C3=COC=C3
  • InChI=1S/C21H17ClN2O6/c22-15-4-5-18(17(9-15)21(27)28)24-20(26)12-30-11-19(25)23-16-3-1-2-13(8-16)14-6-7-29-10-14/h1-10H,11-12H2,(H,23,25)(H,24,26)(H,27,28)
  • Key:BGGMLMAPVODXAU-UHFFFAOYSA-N

References

  1. Jeong BY, Uddin MJ, Park JH, Lee JH, Lee HB, Miyata T, Ha H (2016). "Novel Plasminogen Activator Inhibitor-1 Inhibitors Prevent Diabetic Kidney Injury in a Mouse Model". PLOS ONE. 11 (6): e0157012. Bibcode:2016PLoSO..1157012J. doi:10.1371/journal.pone.0157012. PMID 27258009.
  2. Eren M, Place AT, Thomas PM, Flevaris P, Miyata T, Vaughan DE (September 2017). "PAI-1 is a critical regulator of FGF23 homeostasis". Science Advances. 3 (9): e1603259. Bibcode:2017SciA....3E3259E. doi:10.1126/sciadv.1603259. PMID 28924605. S2CID 13059562.
  3. Hosaka S, Yamada T, Takahashi K, Dan T, Kaneko K, Kodama S, et al. (2020). "Inhibition of Plasminogen Activator Inhibitor-1 Activation Suppresses High Fat Diet-Induced Weight Gain via Alleviation of Hypothalamic Leptin Resistance". Frontiers in Pharmacology. 11: 943. doi:10.3389/fphar.2020.00943. PMID 32670063.
  4. Kuru Bektaşoğlu P, Koyuncuoğlu T, Akbulut S, Akakın D, Eyüboğlu İP, Erzik C, et al. (December 2021). "Neuroprotective Effect of Plasminogen Activator Inhibitor-1 Antagonist in the Rat Model of Mild Traumatic Brain Injury". Inflammation. 44 (6): 2499–2517. doi:10.1007/s10753-021-01520-0. PMID 34460025. S2CID 236584848.
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