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.
Invest Ophthalmol Vis Sci. 2021 Oct 4;62(13):7.
Neutrophil-Derived Proteases Contribute to the Pathogenesis of Early Diabetic Retinopathy
Alvelestat (AZD9668) purchased from AbMole
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 |
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.
Related Elastase Products |
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Ala-Ala-Pro-Val-chloromethylketone
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases. |
MeOSuc-Ala-Ala-Pro-Met-AMC
MeOSuc-Ala-Ala-Pro-Met-AMC is a peptide substrate of elastases and chymotrypsin-like serine peptidases. |
Suc-Ala-Ala-Pro-Val-AMC
Suc-Ala-Ala-Pro-Val-AMC, a tetrapeptide, is an elastasesubstrate. |
Suc-Ala-Ala-Ala-AMC
Suc-Ala-Ala-Ala-AMC is a peptide substrate of elastase or elastase-like. |
Suc-Ala-Pro-Ala-AMC
Suc-Ala-Pro-Ala-AMC is a tripeptide substrate of elastase. |
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