research use only

Alvelestat (AZD9668) Serine Protease inhibitor

Name: Alvelestat (AZD9668)
Brand: Selleck Chemicals
SKU: S7218
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S7218

Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and K_i of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. This compound is in Phase 2.

Chemical Structure

Molecular Weight: 545.53

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.79%

99.79

Related Targets	HDAC Caspase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Proteasome Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin Carboxypeptidase SGK Aminopeptidase 3C-Like Protease PSMA PGDS GOT
Related Products	Leupeptin Hemisulfate PMSF Nafamostat mesilate (FUT-175) Sivelestat AEBSF HCl Sivelestat sodium tetrahydrate Gabexate Mesylate UK-371804 HCl Ulinastatin Fulacimstat FOY251 Antithrombin III/ATIII Antibody [F5E18] Neutrophil Elastase Antibody [N21P16] Sebetralstat PSA/KLK3 Antibody [H22B24] Sivelestat sodium LONP1 Antibody [L16G15] Granzyme B Antibody [B18E4] HAI-1 Antibody [K13J21] Upamostat (WX-671) CLPX Antibody [C16E7] ZK824859 Mast Cell Chymase (C-terminal) Antibody [G3B5] Kallikrein 8/KLK8 Antibody [K4H12]

Chemical Information, Storage & Stability

Molecular Weight	545.53	Formula	C₂₅H₂₂F₃N₅O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	848141-11-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Avelestat			Smiles	CC1=C(C=C(C(=O)N1C2=CC=CC(=C2)C(F)(F)F)C(=O)NCC3=NC=C(C=C3)S(=O)(=O)C)C4=CC=NN4C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (183.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.58mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	neutrophil elastase ^[1] (Cell-free assay) 9.4 nM(Ki) neutrophil elastase ^[1] (Cell-free assay) 12 nM
In vitro	Alvelestat (AZD9668) inhibits plasma NE activity in zymosan-stimulated whole blood, and also inhibits NE activity on the surface of stimulated polymorphonuclear cells and in the supernatant of primed, stimulated cells. ^[1]
In vivo	In mice and rats, Alvelestat (AZD9668) (p.o.) prevents human NE-induced lung injury. In a mouse model of smoke-induced airway inflammation, it significantly reduces the number of BAL neutrophils and BAL IL-1β. In a guinea pig chronic smoke model, this compound prevents airspace enlargement and small airway wall remodeling in guinea pigs in response to chronic tobacco smoke exposure. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/21791628/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01214122	Withdrawn	Pharmacokinetics\|Pharmacodynamics	AstraZeneca	November 2010	Phase 1
NCT01161355	Completed	Healthy	AstraZeneca	June 2010	Phase 1
NCT01147549	Completed	Healthy	AstraZeneca	June 2010	Phase 1
NCT01035411	Completed	Chronic Obstructive Pulmonary Disease	AstraZeneca	November 2009	Phase 1
NCT01034982	Completed	Chronic Obstructive Pulmonary Disease	AstraZeneca	November 2009	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):