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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
| 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.
| Molecular Weight | 545.53 |
| Formula | C25H22F3N5O4S |
| CAS Number | 848141-11-7 |
| Purity | >99% |
| Solubility | DMSO ≥ 60 mg/mL |
| Storage | at -20°C |
| Related Elastase Products |
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| DMP 777
DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor. |
| BAY-85-8501
BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM. |
| Sivelestat
Sivelestat (ONO5046; LY544349; EI546) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. |
| GW311616 hydrochloride
GW311616 HCl (GW311616A) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. |
| GW311616
GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. |
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