GW311616 structure
|
Common Name | GW311616 | ||
---|---|---|---|---|
CAS Number | 198062-54-3 | Molecular Weight | 397.53 | |
Density | N/A | Boiling Point | 604.3ºC at 760mmHg | |
Molecular Formula | C19H31N3O4S | Melting Point | N/A | |
MSDS | N/A | Flash Point | 319.3ºC |
Use of GW311616GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM; free base form of GW311616A.IC50 value: 22 nM [1]Target: neutrophil elastaseThe 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.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic. |
Name | (3aR,6S,6aS)-4-methylsulfonyl-1-[(E)-4-piperidin-1-ylbut-2-enoyl]-6-propan-2-yl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one |
---|---|
Synonym | More Synonyms |
Description | GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM; free base form of GW311616A.IC50 value: 22 nM [1]Target: neutrophil elastaseThe 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.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic. |
---|---|
Related Catalog | |
References |
Boiling Point | 604.3ºC at 760mmHg |
---|---|
Molecular Formula | C19H31N3O4S |
Molecular Weight | 397.53 |
Flash Point | 319.3ºC |
PSA | 86.38000 |
LogP | 2.76850 |
Vapour Pressure | 7.06E-15mmHg at 25°C |
Storage condition | 2-8℃ |
Hazard Codes | Xi: Irritant; |
---|---|
Risk Phrases | R36/37/38 |
Safety Phrases | S26 |
(3S,3AS,6AR)-3-ISOPROPYL-1-(METHANESULFONYL)-4-[4-(1-PIPERIDINYL)-2(E)-BUTENOYL]PERHYDROPYRROLO[3,2B]PYRROL-2(1H)-ONE HYDROCHLORIDE |
GW311616 |