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Chemical Structure| 848141-11-7 Chemical Structure| 848141-11-7

Structure of Alvelestat
CAS No.: 848141-11-7

Chemical Structure| 848141-11-7

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Alvelestat is an inhibitor of neutrophil elastase (NE) with the pIC50 of 7.9.

Synonyms: AZD9668; Avelestat

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Product Details of Alvelestat

CAS No. :848141-11-7
Formula : C25H22F3N5O4S
M.W : 545.53
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
Synonyms :
AZD9668; Avelestat
MDL No. :MFCD26960961
InChI Key :QNQZWEGMKJBHEM-UHFFFAOYSA-N
Pubchem ID :46861623

Safety of Alvelestat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Porcine aortic valve interstitial cells (pVICs) 40 nmol/L 24 hours To investigate the effects of Alvelestat on inflammation, apoptosis, and calcification in pVICs. Results showed that Alvelestat inhibited osteogenic differentiation, inflammation, and apoptosis in pVICs. PMC8994374
Human neutrophils 10 µM 1-hour pretreatment followed by 4-hour stimulation To evaluate the effect of Alvelestat on MSU and PMA-induced neutrophil extracellular trap (NET) formation. Results showed that Alvelestat effectively inhibited NET formation. PMC11719704
Human neutrophils 10 µM 1-hour pretreatment followed by 4-hour stimulation To evaluate the effect of Alvelestat on MSU and PMA-induced neutrophil extracellular trap (NET) formation. Results showed that Alvelestat effectively inhibited NET formation. PMC11719704
Porcine islets 0–25 μM 24 hours To evaluate the inhibitory effect of alvelestat against the cytotoxicity of neutrophil elastase (NE). Results showed that 5 and 25 μM alvelestat recovered the NE-induced decrease in islet viability. PMC9330829

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Apoe−/− mice Western diet-induced aortic valve calcification model Oral 3 mg/kg Once a week for 16 weeks To investigate the effects of Alvelestat on aortic valve calcification. Results showed that Alvelestat alleviated valve thickening, reduced the expression of NE and α-SMA, and improved heart function. PMC8994374
Mice Hydrochloric acid aspiration-induced acute lung injury model Subcutaneous injection 5 mg/kg Immediately after acid aspiration, observed for 12 hours To evaluate the protective effect of Alvelestat on hydrochloric acid aspiration-induced acute lung injury. Results showed that Alvelestat significantly reduced NET formation in lung tissues, decreased inflammatory cytokine levels, and improved lung histopathology. PMC5788598

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01161355 Healthy PHASE1 COMPLETED 2025-06-10 Research Site, Ruddington, Not... More >>tingham, United Kingdom|Research Site, London, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.17mL

1.83mL

0.92mL

18.33mL

3.67mL

1.83mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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