N6022_1208315-24-5_DataSheet_MedChemExpress
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Product Name:
N6022CAS No.:
1208315-24-5Cat. No.:
HY-14984
Product Data Sheet
MWt:
414.46Formula:
C24H22N4O3Purity :>98%
Solubility:
DMSO
Mechanisms:
Biological Activity:
N6022is a potent,selective,reversible,and efficacious S-Nitrosoglutathione reductase(GSNOR) Pathways:Others; Target:GSNOR N6022 is a potent, selective, reversible, and efficacious S Nitrosoglutathione reductase(GSNOR)
inhibitor(IC50=10 nM) which is currently undergoing clinical development.
IC50 value: 10 nM [1]
Target: GSNOR in vitro: N6022 is a tight-binding, specific, and fully reversible inhibitor of GSNOR with an IC(50) of 8nM and a K(i) of 2.5 nM. We accounted for the fact that the NAD(+)- and NADH-dependent oxidation and reduction reactions, catalyzed by GSNOR are bisubstrate in nature in our calculations. N6022binds in the GSNO substrate binding pocket like a competitive inhibitor, although in kinetic assays it behaves with a mixed uncompetitive mode of inhibition (MOI) toward the GSNO substrate and a References:
[1]. Sun X, et al. Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement. Bioorg Med Chem Lett. 2011 Jun
15;21(12):3671-5 mixed competitive MOI toward the formaldehyde adduct, S-hydroxymethylglutathione (HMGSH) [3].in vivo:Sprague-Dawley rats were given 2, 10 or 50 mg/kg/day N6022 via IV administra...
15;21(12):36715.[2]. Colagiovanni DB, et al. A nonclinical safety and pharmacokinetic evaluation of N6022: a first-in-class S-nitrosoglutathione reductase inhibitor for the treatment of asthma. Regul Toxicol Pharmacol.
2012 Feb;62(1):115-24.[3]. Green LS, et al. Mechanism of inhibition for N6022, a first-in-class drug targeting S-
nitrosoglutathione reductase. Biochemistry. 2012 Mar 13;51(10):2157-68.Caution: Not fully tested. For research purposes only
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