Tiplaxtinin

• Description :

  Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM[1].

• CAS Number :

  [393105-53-8]

• Product Name Alternative :

  PAI-039; Tiplasinin

• UNSPSC :

  12352005

• Hazard Statement :

  H302+H312, H315, H318, H411

• Target :

  Apoptosis; PAI-1

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Metabolic Enzyme/Protease

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Metabolic Disease; Cancer

• Assay Protocol :

  https://www.medchemexpress.com/Tiplaxtinin.html

• Concentration :

  10mM

• Purity :

  99.03

• Solubility :

  DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

• Smiles :

  O=C(C(O)=O)C1=CN(CC2=CC=CC=C2)C(C1=C3)=CC=C3C4=CC=C(OC(F)(F)F)C=C4

• Molecular Formula :

  C24H16F3NO4

• Molecular Weight :

  439.38

• Precautions :

  H302+H312, H315, H318, H411

• References & Citations :

  [1]Hennan JK, et al. Effect of Tiplaxtinin (PAI-039), an orally bioavailable PAI-1 antagonist, in a rat model of thrombosis. J Thromb Haemost. 2008 Sep;6 (9) :1558-64.|[2]Gomes-Giacoia E, et al. Targeting plasminogen activator inhibitor-1 inhibits angiogenesis and tumor growth in a human cancer xenograft model. Mol Cancer Ther. 2013 Dec;12 (12) :2697-708.|[3]Hennan JK, et al. Evaluation of PAI-039 [{1-benzyl-5-[4- (trifluoromethoxy) phenyl]-1H-indol-3-yl} (oxo) acetic acid], a novel plasminogen activator inhibitor-1 inhibitor, in a canine model of coronary artery thrombosis. J Pharmacol Exp Ther. 2005 Aug;314 (2) :

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported