1421446-45-8

Basic information

• Product Name: C₂₄H₃₀N₂O₄
• CAS NO: 1421446-45-8
• Molecular Weight: 410.513
• Mol File: 1421446-45-8.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: C₂₄H₃₀N₂O₄(CAS DataBase Reference)
• NIST Chemistry Reference: C₂₄H₃₀N₂O₄(1421446-45-8)
• EPA Substance Registry System: C₂₄H₃₀N₂O₄(1421446-45-8)

Safety Data

• Hazardous Substances Data: 1421446-45-8(Hazardous Substances Data)

Upstream product

• 98778-71-3 cis-(2S,5S)-2,5-dimethylpiperazine dihydrobromide 
• 5437-45-6 Benzyl bromoacetate 

Relevant articles and documents

Development of new cyclic plasmin inhibitors with excellent potency and selectivity

The trypsin-like serine protease plasmin is a target for the development of antifibrinolytic drugs for use in cardiac surgery with cardiopulmonary bypass or organ transplantations to reduce excessive blood loss. The optimization of our recently described substrate-analogue plasmin inhibitors, which were cyclized between their P3 and P2 side chains, provided a new series with improved efficacy and excellent selectivity. The most potent inhibitor 8 binds to plasmin with an inhibition constant of 0.2 nM, whereas Ki values >1 μM were determined for nearly all other tested trypsin-like serine proteases, with the exception of trypsin, which is also inhibited in the nanomolar range. Docking studies revealed a potential binding mode in the widely open active site of plasmin that explains the strong potency and selectivity profile of these inhibitors. The dialkylated piperazine-linker segment contributes to an excellent solubility of all analogues. Based on their overall profile the presented inhibitors are well suited for further development as injectable antifibrinolytic drugs.