GW 311616A

GW 311616A is an inhibitor of neutrophil elastase (IC50 = 100 nM). It is selective for neutrophil elastase (IC50 = 22 nM for the human enzyme) over trypsin, cathepsin G, and plasmin (IC50s = >100 µM for all), as well as chymotrypsin and tissue plasminogen activator (IC50s = >3 µM for both), in cell-free assays. GW 311616A (20 µM) inhibits the formation of neutrophil extracellular traps (NETs) induced by phorbol 12-myristate 13-acetate (PMA, Cay-10008014) in isolated human neutrophils. It inhibits intraneutrophil elastase activity in isolated dog blood six hours after administration of a 0.22 mg/kg dose. GW 311616A also inhibits neutrophil elastase in the liver in a mouse model of liver ischemia-reperfusion injury when administered at a dose of 2 mg/kg.Formal Name: (3S,3aS,6aR)-hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-[(2E)-1-oxo-4-(1-piperidinyl)-2-buten-1-yl]-pyrrolo[3,2-b]pyrrol-2(1H)-one, monohydrochloride. CAS Number: 197890-44-1. Molecular Formula: C19H31N3O4S . HCl. Formula Weight: 434.0. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.25 mg/ml, Ethanol: 10 mg/ml. SMILES: O=C(N1CC[C@](N2S(C)(=O)=O)([H])[C@]1([H])[C@H](C(C)C)C2=O)/C=C/CN3CCCCC3.Cl. InChi Code: InChI=1S/C19H31N3O4S.ClH/c1-14(2)17-18-15(22(19(17)24)27(3,25)26)9-13-21(18)16(23)8-7-12-20-10-5-4-6-11-20,/h7-8,14-15,17-18H,4-6,9-13H2,1-3H3,1H/b8-7+,/t15-,17+,18-,/m1./s1. InChi Key: UFCZUKYPBPXODT-OFTZGUNKSA-N.