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GW311616 HCl (GW311616A) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. 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). GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic.
| Molecular Weight | 433.99 |
| Formula | C19H31N3O4S.HCl |
| CAS Number | 197890-44-1 |
| Solubility (25°C) | DMSO 10 mM |
| 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
GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM and Ki value of 0.31 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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