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TM 5275
Axon 2344
- Parent CAS: 1103928-13-7
Purity:
99%
- Soluble in DMSO
- MF: C28H27ClN3NaO5
- MW: 543.97
Description
TM 5275 is a selective, orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1/SERPINE1) with an IC50 value of 6.95 μM in a tPA-dependent peptide hydrolysis assay. It prolongs tPA retention, enhances vascular endothelial plasmin generation and modulates PAI-1/LRP1-dependent macrophage migration.
PAI-1 suppresses fibrinolysis and contributes to thrombosis, inflammation and vascular remodeling. TM 5275 is useful for studying PAI-1-dependent antithrombotic mechanisms and inflammatory cell migration without increasing bleeding liability in reported models.
Key Features
- Selective PAI-1/SERPINE1 inhibitor
- IC50: 6.95 μM in tPA-dependent assays
- Enhances plasmin generation on vascular endothelial cells
- Modulates PAI-1/LRP1-mediated macrophage migration
Applications
- Fibrinolysis and thrombosis research
- PAI-1 pharmacology
- Vascular endothelial biology
- Inflammatory macrophage migration assays
More Information
| Parent CAS No. | 1103928-13-7 |
|---|---|
| Chemical Name | Sodium 2-(2-(2-(4-benzhydrylpiperazin-1-yl)-2-oxoethoxy)acetamido)-5-chlorobenzoate |
| SMILES | C([O-])(=O)C1=CC(Cl)=CC=C1NC(COCC(N1CCN(C(C2=CC=CC=C2)C2=CC=CC=C2)CC1)=O)=O.[Na+] |
| MFCD | N.A. |
| InChi | InChI=1S/C28H28ClN3O5.Na/c29-22-11-12-24(23(17-22)28(35)36)30-25(33)18-37-19-26(34)31-13-15-32(16-14-31)27(20-7-3-1-4-8-20)21-9-5-2-6-10-21;/h1-12,17,27H,13-16,18-19H2,(H,30,33)(H,35,36);/q;+1/p-1 |
| InChiKey | JSHSGBIWNPQCQZ-UHFFFAOYSA-M |
| CID | 53240409 |
| Short Description | PAI-1 inhibitor |
References
- Y. Izuhara et al. A novel inhibitor of plasminogen activator inhibitor-1 provides antithrombotic benefits devoid of bleeding effect in nonhuman primates. J. Cereb. Blood Flow Metab. 2010, 30, 904-912.
- H. Yasui et al. TM5275 prolongs secreted tissue plasminogen activator retention and enhances fibrinolysis on vascular endothelial cells. Thromb. Res. 2013, 132, 100-105.
- A. Ichimura et al. A small molecule inhibitor to plasminogen activator inhibitor 1 inhibits macrophage migration. Arterioscler. Thromb. Vasc. Biol. 2013, 33, 935-942.
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