Tiplaxtinin

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

Product Specifications

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) :