Gabexate (mesylate)

Gabexate is a competitive inhibitor of serine proteases that inhibits human thrombin, urokinase, plasmin, and Factor Xa (Kis = 0.97, 1.3, 1.6, and 8.5 µM, respectively)., It also inhibits bovine thrombin, Factor Xa, and trypsin, and porcine plasma kallikrein (Kis = 1.4, 2.1, 2.6, and 0.2 µM, respectively)., In vitro, gabexate inhibits clotting activity of thrombin (IC50 = 10 µM). In vivo, it inhibits fibrin formation in rats when administered at a continuous infusion of 120 µmol/kg per hour. Gabexate inhibits LPS-stimulated TNF-alpha production from monocytes by inhibiting binding of NF-kappaB and activator protein 1 (AP-1) to target sites and inducing degradation of IkappaBalpha.Formal Name: 4-[[6-[(aminoiminomethyl)amino]-1-oxohexyl]oxy]-benzoic acid ethyl ester, monomethanesulfonate. CAS Number: 56974-61-9. Molecular Formula: C16H23N3O4 . CH3SO3H. Formula Weight: 417.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml. lambdamax: 236 nm. SMILES: O=C(OCC)C1=CC=C(OC(CCCCCNC(N)=N)=O)C=C1.O=S(C)(O)=O. InChi Code: InChI=1S/C16H23N3O4.CH4O3S/c1-2-22-15(21)12-7-9-13(10-8-12)23-14(20)6-4-3-5-11-19-16(17)18,1-5(2,3)4/h7-10H,2-6,11H2,1H3,(H4,17,18,19),1H3,(H,2,3,4). InChi Key: DNTNDFLIKUKKOC-UHFFFAOYSA-N.