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Submit ReviewTiplaxtinin 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.
Tiplaxtinin is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 439.38 |
Formula | C24H16F3NO4 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 393105-53-8 |
PubChem ID | 6450819 |
InChI Key | ODXQFEWQSHNQNI-UHFFFAOYSA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 43.94 | 100 | |
ethanol | 43.94 | 100 |
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.
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 |
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
If you know of a relevant reference for Tiplaxtinin, please let us know.
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
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
Do you know of a great paper that uses Tiplaxtinin from Tocris? Please let us know.
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