GSK2190915

GSK2190915 is a selective inhibitor of human 5-lipoxygenase-activating protein (FLAP, IC50 = 2.9 nM). It is selective for FLAP over 5-, 12-, and 15-lipoxygenase, leukotriene A4 (LTA4) hydrolase, LTC4 synthase, COX-1, and COX-2 (IC50s = >10 µm for all). GSK2190915 inhibits production of LTB4 induced by the calcium ionophore A23187 (Cay-11016) in isolated whole blood from human, rat, and mouse (IC50s = 436, 223, and 148 nM, respectively). It decreases increases in the levels of cysteinyl leukotriene (CysLT) and LTB4 induced by lung instillation of A23187 in the bronchoalveolar lavage fluid (BALF) of rats when administered at doses of 1 and 3 mg/kg. GSK219095 (3 mg/kg) also reduces increases in the levels of CysLT, LTB4, myeloperoxidase (MPO), and plasma protein extravasation in a mouse model of peritonitis induced by zymosan in mice.Formal Name: 3-[(1,1-dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-alpha,alpha-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-1H-indole-2-propanoic acid. CAS Number: 936350-00-4. Synonyms: AM803. Molecular Formula: C38H43N3O4S. Formula Weight: 637.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Methanol: soluble. lambdamax: 215, 262 nm. SMILES: CC1=CN=C(COC2=CC(C(SC(C)(C)C)=C(CC(C)(C)C(O)=O)N3CC4=CC=C(C5=CN=C(OCC)C=C5)C=C4)=C3C=C2)C=C1. InChi Code: InChI=1S/C38H43N3O4S/c1-8-44-34-18-14-28(22-40-34)27-12-10-26(11-13-27)23-41-32-17-16-30(45-24-29-15-9-25(2)21-39-29)19-31(32)35(46-37(3,4)5)33(41)20-38(6,7)36(42)43/h9-19,21-22H,8,20,23-24H2,1-7H3,(H,42,43). InChi Key: DFQGDHBGRSTTHX-UHFFFAOYSA-N.