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TM5275 sodium is an orally available, potent and selective plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates. TM5275 enhances the time-dependent accumulation of plasminogen as well as the dissolution of fibrin clots on and around the tPA-GFP-expressing cells. Active PAI-1 in cell culture media is significantly decreased in cells treated with 100 μM TM5275 compared to control treatment.
TM5275 exhibits a favorable pharmacokinetics profile and very low toxicity to mice and rats. TM5275 (5 mg/kg) combined with tPA (0.3 mg/kg) significantly enhances the antithrombotic effect of tPA (0.3 mg/kg) alone and provides a benefit similar to that of a high tPA dose (3 mg/kg).
| Molecular Weight | 543.97 |
| Formula | C28H27ClN3O5.Na |
| CAS Number | 1103926-82-4 |
| Solubility (25°C) | DMSO ≥ 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PAI-1 Products |
|---|
| BC-11 hydrobromide
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). |
| Glutaryl-Gly-Arg-AMC
Glutaryl-Gly-Arg-AMC is a peptide substrate of urokinase plasminogen activator (uPA). |
| GGACK
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor. |
| PPACK
PPACK is a plasminogen activator (rt-PA) inhibitor. |
| Anecortave acetate
Anecortave acetate is a potent ocular vascular inhibitor that inhibits angiogenic factor-induced neointima formation and also increases fibrinogen activator inhibitor 1 (PAI-1) mRNA expression.Anecortave acetate can be used in studies related to ocular neovascularization diseases. |
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