1. Metabolic Enzyme/Protease
  2. Elastase
  3. Alvelestat

Alvelestat (Synonyms: AZD9668)

Cat. No.: HY-15651 Purity: 99.88%
Handling Instructions

Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.

For research use only. We do not sell to patients.

Alvelestat Chemical Structure

Alvelestat Chemical Structure

CAS No. : 848141-11-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
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10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
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100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM[1].

IC50 & Target

pIC: 7.9 nM; Ki: 9.4 nM; Kd: 9.5 nM (neutrophil elastas)[1]

In Vitro

Alvelestat (20 μg/mL; 16 hours; HBE and A549 cells) treatment decreases cells death and decreases the levels of IL-1β, IL-6, and TNF-α in vitro[2].

Cell Viability Assay[2]

Cell Line: Human bronchial epithelial cells (HBE) and human alveolar epithelial cells (A549)
Concentration: 20 μg/mL
Incubation Time: 16 hours
Result: Decreased cytotoxicity and inflammatory responses.
In Vivo

Alvelestat (1-10 mg/kg; oral administration; twice daily; for 4 days; Female BALB/cJBomTac mice) treatment reduces the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β[1].

Animal Model: Female BALB/cJBomTac mice exposed to smoke cigarette smoke[1]
Dosage: 1 mg/kg , 3 mg/kg , 6 mg/kg , 10 mg/kg
Administration: Oral administration; twice daily; for 4 days
Result: Reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β.
Clinical Trial
Molecular Weight

545.53

Formula

C₂₅H₂₂F₃N₅O₄S

CAS No.

848141-11-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (60.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.88%

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Keywords:

AlvelestatAZD9668AZD 9668AZD-9668ElastaseInhibitorinhibitorinhibit

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Alvelestat
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HY-15651
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