Izoquinolin-1-ylamine

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

Purity: 95%

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.