Sivelestat (sodium salt hydrate)

Sivelestat is an inhibitor of neutrophil elastase (IC50 = 44 nM for the human enzyme). It is selective for neutrophil elastase over trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G at 100 µM. Sivelestat inhibits the formation of neutrophil extracellular traps (NETs) induced by ionomycin (Cay-10004974, Cay-11932) in isolated mouse neutrophils. It decreases LPS-induced NF-kappaB nuclear translocation in isolated rat pulmonary microvascular endothelial cells (PMVECs) at 50 mM. Sivelestat (10 mg/kg) reduces pulmonary edema, increases in the number of cells in the lung tissue positive for myeloperoxidase (MPO), a marker of neutrophil infiltration, and the severity of lung injury in a rat model of LPS-induced acute lung injury.Formal Name: 2,2-dimethyl-propanoic acid, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester, monosodium salt, tetrahydrate. CAS Number: 201677-61-4. Synonyms: LY544349, ONO-5046. Molecular Formula: C20H21N2O7S . Na [4H2O]. Formula Weight: 528.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 15 mg/ml, Ethanol: 0.3 mg/ml, PBS (pH 7.2): 2 mg/ml. lambdamax: 210 nm. SMILES: O=S(C1=CC=C(OC(C(C)(C)C)=O)C=C1)(NC2=C(C(NCC([O-])=O)=O)C=CC=C2)=O.[Na+].O.O.O.O. InChi Code: InChI=1S/C20H22N2O7S.Na.4H2O/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24,,,,,/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24),,4*1H2/q,+1,,,,/p-1. InChi Key: PLHREJBSQUSUCW-UHFFFAOYSA-M.