- Sivelestat sodium salt
- ARP 100
| AlvelestatNE inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.67%
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Chemical structure
| Description | Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with pIC50 value of 7.9 | |||||
| Targets | NE | |||||
| IC50 | (pIC50=7.9,Ki=4.9 nM) | |||||
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| Cas No. | 848141-11-7 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)pyridin-2-yl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide | ||
| Canonical SMILES | CC(N1C2=CC=CC(C(F)(F)F)=C2)=C(C3=CC=NN3C)C=C(C1=O)C(NCC4=NC=C(S(C)(=O)=O)C=C4)=O | ||
| Formula | C25H22F3N5O4S | M.Wt | 545.53 |
| Solubility | ≥27.3mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Alvelestat is an orally bioavailable inhibitor of neutrophil elastase (NE) with pIC50 value of 7.9[1].
The reversible NE inhibitor, alvelestat, is developed for treating the neutrophil-driven inflammatory lung diseases such as bronchiectasis and chronic obstructive pulmonary diseas. Alvelestat shows high affinity with human NE with a Ki value of 9.4nM. It is more than 600-fold selective for human NE over other serine proteases. In the whole-blood and cell- associated and explosive-release assays, alvelestat shows pIC50 values of 7.36, 7.32 and 7.3, respectively. In the acute lung injury model, administration of alvelestat significantly reduces the levels of hemoglobin and BAL hydroxyproline induced by human NE. In the smoke-induced airway inflammation model, alvelestat reduces both BAL neutrophils and IL-1β markedly. Furthermore, alvelestat can relieve inflammation and inhibit smoke-induced increases in lavage neutrophils and macrophages in a model of chronic smoke-induced inflammation and emphysema [1].
References:[1] Stevens T, Ekholm K, Gränse M, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. Journal of Pharmacology and Experimental Therapeutics, 2011, 339(1): 313-320.
