搜档网
当前位置:搜档网 › Alvelestat_848141-11-7_DataSheet_MedChemExpress

Alvelestat_848141-11-7_DataSheet_MedChemExpress

Alvelestat_848141-11-7_DataSheet_MedChemExpress

Product Name:

Alvelestat CAS No.:

848141-11-7Cat. No.:

HY-15651

Product Data Sheet

MWt:

545.53Formula:

C25H22F3N5O4S Purity :>98%

Solubility:

DMSO

y Mechanisms:

Biological Activity:

Alvelestat (AZD9668)is a novel oral inhibitor of neutrophil elastase (NE)with the pIC50of 79for Pathways:Metabolism/Protease; Target:Elastase Alvelestat (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9 for

Human NE.

IC50 Value: 7.9 ± 0.12 (pIC50, Human NE); 4.9 nM (Ki value, Human NE) [1]

Target: Neutrophil elastase in vitro: AZD9668 had a high binding affinity for human NE (KD = 9.5 nM) and potently inhibited NE activity. The calculated pIC50 (IC50) and Ki values for AZD9668 for human NE were 7.9 (12 nM)and 4.9 nM, respectively. In contrast to earlier NE inhibitors, the interaction between AZD9668 and NE was rapidly reversible. AZD9668 was also highly selective for NE over other neutrophil-derived serine proteases. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-References:

[1]. Stevens T, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of

neutrophil elastase. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20.[2]. Kuna P, et al. AZD9668, a neutrophil elastase inhibitor, plus ongoing budesonide/formoterol in p y ,p y y

stimulated whole blood. In isolated human polymorphonuclear cells, AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells.AZD9...

patients with COPD. Respir Med. 2012 Apr;106(4):531-9.[3]. Vogelmeier C, et al. A randomised, placebo-controlled, dose-finding study of AZD9668, an oral inhibitor of neutrophil elastase, in patients with chronic obstructive pulmonary disease treated with

tiotropium. COPD. 2012 Apr;9(2):111-20.[4]. Gunawardena KA, et al. Pharmacokinetics and safety of AZD9668, an oral neutrophil elastase inhibitor, in healthy volunteers and patients with COPD. Int J Clin Pharmacol Ther. 2013

Apr;51(4):288-304....

Caution: Not fully tested. For research purposes only

Medchemexpress LLC

https://www.sodocs.net/doc/0a4948581.html,

18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S A

E m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m

相关主题