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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 10 mM|
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GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.
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