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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.
|Storage||Store at +4°C|
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|
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 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||2.22 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|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TM 5441, please let us know.
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