Nitric oxide synthase (inducible) Inhibitor
Potent inhibitor of endothelial nitric oxide synthase, neuronal nitric oxide synthase (this isoforms are constitutively expressed and are regulated by Ca2+ ion and calmodulin) and inducible nitric oxide synthase (this isoform which is induced by exogenous or endogenous inflammatory stimuli, notably endotoxins (LPS) and cytokines (IL-I etc.), is not regulated by Ca2+ ion flux) with IC50 values of 10.6 μM, 50 μM and 9.9 μM respectively.
OTAVAchemicals Catalogue Number: 1055516
CAS Registry Number: 1532-84-9
Ref.: W. K. Hagmann et al. Substituted 2-Aminopyridines as Inhibitors of Nitric Oxide Synthases. Bioorg. Med. Chem. Lett. 10 (2000) 1975-1978.
Abstract: A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC50 of 28 nM.