TM-5275 (TM5275) is a potent, orally active PAI-1 (plasminogen activator inhibitor-1) inhibitor with IC50 of 6.95 uM.
TM-5275 does not interfere with other serpin/serine protease systems (α1-antitrypsin/trypsin and α2-antiplasmin/plasmin).
TM-5275 exhibits antithrombotic effect in an arterial venous shunt thrombosis model (1-10 mg/kg).
TM-5275 blocks TGF-β1-induced lung fibrosis, and induces apoptosis in both myofibroblasts (TGF-β1-treated) and naive (TGF-β1-untreated) human lung fibroblasts.
Physicochemical Properties
M.Wt
543.98
Formula
C28H27ClN3NaO5
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
2-[2-[2-(4-Benzhydrylpiperazin-1-yl)-2-oxoethoxy]acetamido]-5-chlorobenzoic acid sodium salt
References
1. Izuhara Y, et al. J Cereb Blood Flow Metab. 2010 May;30(5):904-12.
2. Huang WT, et al. Am J Respir Cell Mol Biol. 2012 Jan;46(1):87-95.
3. Tashiro Y, et al. Blood. 2012 Jun 28;119(26):6382-93.
