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Alvelestat (AZD9668)

Cat. No. M5402
Alvelestat (AZD9668) Structure
Synonym:

AZD9668

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 210  USD210 In stock
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Quality Control & Documentation
Biological Activity

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

Product Citations
Chemical Information
Molecular Weight 545.53
Formula C25H22F3N5O4S
CAS Number 848141-11-7
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yamada K, et al. Mol Genet Metab. Elevation of pivaloylcarnitine by sivelestat sodium in two children.

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