Sivelestat sodium salt is a selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. Inhibits NF-κB activation and LTB4-induced neutrophil transmigration in vitro. Significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo.
| Molecular Weight | 456.44 |
| Formula | C20H21N2NaO7S |
| CAS Number | 150374-95-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 22.82 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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