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Cat.No. 5565 - Tiplaxtinin | C24H16F3NO4 | CAS No. 393105-53-8
Description: Plasminogen activator inhibitor-1 (PAI-1) inhibitor
Alternative Names: PAI 039, tiplasinin
Chemical Name: α-Oxo-1-(phenylmethyl)-5-[4-(trifluoromethoxy)phenyl]-1H-indole-3-acetic acid
Purity: ≥98% (HPLC)

Biological Activity

Plasminogen activator inhibitor-1 (PAI-1) inhibitor (IC50 = 2.7 μM). Induces vascular smooth muscle cell apoptosis in vitro and reduces carotid artery neointimal formation in a rat vascular injury model. Promotes thrombolysis in rat and dog models of acute arterial thrombosis. Orally available.

Compound Libraries

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Technical Data

M. Wt 439.38
Formula C24H16F3NO4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 393105-53-8
PubChem ID 6450819
Smiles O=C(C(O)=O)C2=CN(CC3=CC=CC=C3)C1=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 43.94 100
ethanol 43.94 100

Preparing Stock Solutions

The following data is based on the product molecular weight 439.38. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.38 mL 22.76 mL
5 mM 0.46 mL 2.28 mL 4.55 mL
10 mM 0.23 mL 1.14 mL 2.28 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

Safety Datasheet


References are publications that support the products' biological activity.

Elokdah et al (2004) Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization. J.Med.Chem. 47 3491 PMID: 15214776

Simone et al (2015) A small molecule PAI-1 functional inhibitor attenuates neointimal hyperplasia and vascular smooth muscle cell survival by promoting PAI-1 cleavage. Cell.Signal. 27 923 PMID: 25617690

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New Product Guide

New Product Guide (Spring/Summer 2017)

Our new product guide highlights over 130 new products added to the Tocris Bioscience range during the first half of 2017.

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