Alvelestat (AZD9688)

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510254

CAS#: 848141-11-7

Description: Avelestat, also known as AZD9668 and MPH-966, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. AZD9668 has the potential to reduce lung inflammation and the associated structural and functional changes in human diseases.

Chemical Structure

Alvelestat (AZD9688)
CAS# 848141-11-7

Theoretical Analysis

MedKoo Cat#: 510254
Name: Alvelestat (AZD9688)
CAS#: 848141-11-7
Chemical Formula: C25H22F3N5O4S
Exact Mass: 545.13446
Molecular Weight: 545.53
Elemental Analysis: C, 55.04; H, 4.06; F, 10.45; N, 12.84; O, 11.73; S, 5.88

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same Day
25.0mg USD 150.0 Same Day
50.0mg USD 250.0 Same Day
100.0mg USD 450.0 Same Day
200.0mg USD 850.0 Same Day
500.0mg USD 1850.0 Same Day
1.0g USD 2750.0 Same Day
2.0g USD 4650.0 Same Day
5.0g USD 6950.0 2 Weeks
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Synonym: AZD9668; AZD 9668; AZD-9668; MPH966; MPH 966; MPH-966; Alvelestat;

IUPAC/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


InChi Code: InChI=1S/C25H22F3N5O4S/c1-15-20(22-9-10-31-32(22)2)12-21(23(34)30-13-17-7-8-19(14-29-17)38(3,36)37)24(35)33(15)18-6-4-5-16(11-18)25(26,27)28/h4-12,14H,13H2,1-3H3,(H,30,34)

SMILES Code: O=C(C1=CC(C2=CC=NN2C)=C(C)N(C3=CC=CC(C(F)(F)F)=C3)C1=O)NCC4=NC=C(S(=O)(C)=O)C=C4

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 545.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Henriksen PA. The potential of neutrophil elastase inhibitors as anti-inflammatory therapies. Curr Opin Hematol. 2014 Jan;21(1):23-8. doi: 10.1097/MOH.0000000000000001. PubMed PMID: 24241342.

2: Stockley R, De Soyza A, Gunawardena K, Perrett J, Forsman-Semb K, Entwistle N, Snell N. Phase II study of a neutrophil elastase inhibitor (AZD9668) in patients with bronchiectasis. Respir Med. 2013 Apr;107(4):524-33. doi: 10.1016/j.rmed.2012.12.009. Epub 2013 Feb 20. PubMed PMID: 23433769.

3: Gunawardena KA, Gullstrand H, Perrett J. 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. doi: 10.5414/CP201674. PubMed PMID: 23391369.

4: Vogelmeier C, Aquino TO, O'Brien CD, Perrett J, Gunawardena KA. 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. doi: 10.3109/15412555.2011.641803. PubMed PMID: 22458939.

5: Sjö P. Neutrophil elastase inhibitors: recent advances in the development of mechanism-based and nonelectrophilic inhibitors. Future Med Chem. 2012 Apr;4(5):651-60. doi: 10.4155/fmc.12.17. Review. PubMed PMID: 22458683.

6: Elborn JS, Perrett J, Forsman-Semb K, Marks-Konczalik J, Gunawardena K, Entwistle N. Efficacy, safety and effect on biomarkers of AZD9668 in cystic fibrosis. Eur Respir J. 2012 Oct;40(4):969-76. Epub 2012 Jan 20. PubMed PMID: 22267768.

7: Kuna P, Jenkins M, O'Brien CD, Fahy WA. AZD9668, a neutrophil elastase inhibitor, plus ongoing budesonide/formoterol in patients with COPD. Respir Med. 2012 Apr;106(4):531-9. doi: 10.1016/j.rmed.2011.10.020. Epub 2011 Dec 23. PubMed PMID: 22197578.

8: Stevens T, Ekholm K, Gränse M, Lindahl M, Kozma V, Jungar C, Ottosson T, Falk-Håkansson H, Churg A, Wright JL, Lal H, Sanfridson A. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. doi: 10.1124/jpet.111.182139. Epub 2011 Jul 26. PubMed PMID: 21791628