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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)
Citations (1)
Literature (1)

Biological Activity for Tiplaxtinin

Tiplaxtinin is a 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 for Tiplaxtinin

Tiplaxtinin is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Tiplaxtinin

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Tiplaxtinin

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

Preparing Stock Solutions for Tiplaxtinin

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

Select a batch to recalculate based on the batch molecular weight:
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 for Tiplaxtinin

Certificate of Analysis / Product Datasheet
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References for Tiplaxtinin

References are publications that support the biological activity of the product.

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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Keywords: Tiplaxtinin, Tiplaxtinin supplier, thrombolysis, thrombolytic, PAI-1, plasminogen, activator, inhibitors, inhibits, apoptosis, inducers, induces, orally, available, PAI039, PAI, 039, tiplasinin, Plasminogen, Activator, Inhibitor, 1, 5565, Tocris Bioscience

1 Citation for Tiplaxtinin

Citations are publications that use Tocris products. Selected citations for Tiplaxtinin include:

Zhang et al (2020) ACSL3-PAI-1 signaling axis mediates tumor-stroma cross-talk promoting pancreatic cancer progression. Sci Adv 6 PMID: 33127675

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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Angiogenesis in Cancer Poster

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