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Signaling Pathway

Alvelestat

HY-15651

(AZD9668; AZD-9668; AZD 9668)

Alvelestat

Alvelestat Chemical Structure

Alvelestat (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9 for Human NE.

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10 mM * 1 mL in DMSO $156 In-stock
5 mg $130 In-stock
10 mg $210 In-stock
50 mg $750 In-stock
100 mg $1250 In-stock
200 mg Get quote
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Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €153 In-stock
5 mg €127 In-stock
10 mg €206 In-stock
50 mg €735 In-stock
100 mg €1225 In-stock
200 mg Get quote
500 mg Get quote

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Product name: Alvelestat
Cat. No.: HY-15651

Alvelestat Data Sheet

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    Purity: 98.98%

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    DataSheet

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Biological Activity of Alvelestat

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-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.AZD9668 showed good crossover potency to NE from other species [1].
in vivo: Six hundred and fifteen patients were randomised: placebo (302), AZD9668 60 mg bid (313). AZD9668 showed no effect on lung function: change in mean pre-bronchodilator FEV1 versus placebo was 0.01L (95% confidence interval: -0.03, 0.05; p=0.533). AZD9668 did not significantly improve respiratory signs and symptoms, SGRQ-C score or time to first exacerbation. Adverse events were similar for AZD9668 and placebo [2]. AZD9668 was well tolerated at single doses up to 150 mg and multiple doses up to 70 mg twice daily. PK were dose linear; median time to peak plasma concentration was reached at 0.5 - 1.5 hours and the short elimination half-life was consistent with twice daily dosing. Steady state was reached by Day 2 of twice daily dosing with negligible accumulation. Approximately 40% of AZD9668 was eliminated renally as unchanged compound. Ex vivo zymosan-stimulated inhibition of NE activity was dose-dependent, with maximal inhibition achieved at 60 mg [4].
Toxicity: A total of 838 patients were randomised to AZD9668 5 mg bid (212 patients), 20 mg bid (206 patients), 60 mg bid (202 patients) or placebo (218 patients). AZD9668 showed no effect on lung function, respiratory signs and symptoms, QoL or biomarkers [3].
Clinical trial: Phase II study of a neutrophil elastase inhibitor (AZD9668) in patients with bronchiectasis.
 

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 545.53 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H22F3N5O4S
CAS No 848141-11-7
Solvent & Solubility

DMSO: ≥ 33 mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.8331 mL 9.1654 mL 18.3308 mL
5 mM 0.3666 mL 1.8331 mL 3.6662 mL
10 mM 0.1833 mL 0.9165 mL 1.8331 mL

References on Alvelestat

Inhibitor Kit

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