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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 |
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| PAI-039
PAI-039 is an inhibitor of plasminogen activator inhibitor-1 (PAI-1). |
| Loureirin B
Loureirin B is a flavonoid isolated from The blood tree of Pterygophyllum SPP. It is an inhibitor of PAI-1 with IC50 value of 26.10 μM. Loureirin B can inhibit the phosphorylation of KATP, ERK and JNK at the same time, showing an anti-diabetes effect. |
| TM5441
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), with IC50 values between 13.9 and 51.1 μM against several human cancer cell lines. |
| Toddalolactone
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM. |
| AZ3976
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay. |
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