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GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. GW311616 is the free base form of GW311616A. The HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.
GW-311616 (2 mg/kg; oral administration) rapidly abolishes the circulation of neutrophil elastase (NE) in dogs, while >90% inhibition is maintained for 4 days. This prolonged effect is independent to be due to penetration of neutrophils in bone marrow by orally administrated GW-311616. GW-311616 has moderate terminal elimination half-life (t1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively.
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Source | Mol Med Rep (2015). Figure 4. GW311616 |
| Method | proliferation assay | |
| Cell Lines | U937 cells | |
| Concentrations | 150 μmol/l | |
| Incubation Time | 48 h | |
| Results | In the GW311616A.treated group, the rate of apoptosis was enhanced, as compared with the control group |
| Molecular Weight | 397.53 |
| Formula | C19H31N3O4S |
| CAS Number | 198062-54-3 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Elastase Products |
|---|
| Chrysophanol-8-O-β-D-glucopyranoside
Chrysophanol 8-O-glucoside is derived from the root of Rumex acetosa and has moderate elastase inhibitory activity. |
| GW311616 hydrochloride
GW311616 HCl (GW311616A) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. |
| Alvelestat (AZD9668)
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. |
| Sivelestat sodium tetrahydrate
Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse. |
| Sivelestat sodium salt
Sivelestat sodium salt is a selective leukocyte elastase inhibitor. |
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