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
water 2.25 5mM with gentle warming

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

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.

  • 7-TM Receptors
  • Enzymes
  • Enzyme-Linked Receptors
  • Ion Channels
  • Nuclear Receptors
  • Transporters
  • Apoptosis
  • Cell Metabolism
  • Epigenetics
  • Fluorescent Imaging
  • Signal Transduction
  • Stem Cells