TM 5441

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Cat.No. 6194 - TM 5441 | C21H16ClN2NaO6
Description: Plasminogen activator inhibitor-1 (PAI-1) inhibitor
Chemical Name: 5-Chloro-2-[[2-[2-[[3-(3-furanyl)phenyl]amino]-2-oxoethoxy]acetyl]amino]benzoic acid sodium salt
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Plasminogen activator inhibitor-1 (PAI-1) inhibitor (IC50 = 3.58 - 60.3 μM). Increases apoptosis in human cancer cell lines. Reduces senescence and increases lifespan in mouse models of ageing (kl/kl). Inhibits L-NAME (Cat.No. 0665) induced systolic blood pressure increases, telomere length reduction and cardiac hypertrophy in mice. Renoprotective. Orally bioavailable.

Technical Data

M. Wt 450.8
Formula C21H16ClN2NaO6
Storage Store at +4°C
Purity ≥98% (HPLC)
PubChem ID 44250349
InChI Key RDKPAESSEMYFJL-UHFFFAOYSA-M
Smiles O=C(C1=C(C=CC(Cl)=C1)NC(COCC(NC2=CC=CC(C3=COC=C3)=C2)=O)=O)O[Na]

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
Solubility
DMSO 45.08 100

Preparing Stock Solutions

The following data is based on the product molecular weight 450.8. 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 2.22 mL 11.09 mL 22.18 mL
5 mM 0.44 mL 2.22 mL 4.44 mL
10 mM 0.22 mL 1.11 mL 2.22 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Placencio et al (2015) Small molecule inhibitors of plasminogen activator inhibitor-1 elicit anti-tumorigenic and anti-angiogenic activity. PLoS One. 10 PMID: 26207899

Jeong et al (2016) Novel plasminogen activator inhibitor-1 inhibitors prevent diabetic kidney injury in a mouse model. PLoS One. 11 PMID: 27258009

Boe et al (2013) Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence. Circulation. 128 2318 PMID: 24092817

Eren et al (2014) PAI-1-regulated extracellular proteolysis governs senescence and survival in Klotho mice. Proc.Natl.Acad.Sci.USA. 111 7090 PMID: 24778222


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Citations for TM 5441

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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* or download your copy today!

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


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.