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Heteroaryl butanoic acid derivatives as leukotriene A4 hydrolase inhibitors and their preparation
InChi: InChI=1S/C21H26N4O8
EPZ-5676 was used at 1 µM final concentration in vitro and in cellular assays
fibrosis and apoptosis induced by Ang II in mouse model with PAH (pregnancy-associated cardiomyopathy)
very good solubility
Darusentan 9424) Heteroaryl butanoic acid derivatives asDarusentan (Lu 135252) is a selective endothelin receptor A (ET A) receptor antagonist, which binds with a Ki of 1. 4 nM to the ET A receptor and a Ki of 184 nM to ET B receptor, respectively with a 100 fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single site kinetics, exhibiting a Ki of 13 nM. Product information CAS
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