197890-44-1

197890-44-1 structure

Name: GW311616A
Chemical Name: GW311616 hydrochloride
CAS Number: 197890-44-1
Molecular Formula: C₁₉H₃₂ClN₃O₄S
Molecular Weight: 433.993
Catalog: Signaling Pathways Metabolic Enzyme/Protease Elastase
Create Date: 2018-05-28 07:06:22
Modify Date: 2024-01-08 15:04:27
GW311616A(GW311616 Hcl) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.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	GW311616 hydrochloride
Synonyms	GW-311616A (3S,3aS,6aR)-3-Isopropyl-1-(methylsulfonyl)-4-[(2E)-4-(1-piperidinyl)-2-butenoyl]hexahydropyrrolo[3,2-b]pyrrol-2(1H)-one hydrochloride (1:1) 171SKM32U6 MFCD06411566 Pyrrolo[3,2-b]pyrrol-2(1H)-one, hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-[(2E)-1-oxo-4-(1-piperidinyl)-2-buten-1-yl]-, (3S,3aS,6aR)-, hydrochloride (1:1) GW311616 (hydrochloride) GW311616A

Description	GW311616A(GW311616 Hcl) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.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	Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase Research Areas >> Inflammation/Immunology
References	[1]. Macdonald SJ, et al. The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate. Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8.