GW 856553X

GW 856553X is a dual inhibitor of p38alpha and p38beta MAPK (Kis = 0.0079 and 0.025 µM, respectively, in cell-free assays). It is selective for p38alpha and p38beta MAPK over p38gamma and p38delta MAPK when used at a concentration of 10 µM. GW 856553X inhibits LPS-induced TNF-alpha production in isolated rat and human peripheral blood mononuclear cells (PBMCs, IC50s = 0.6 and 0.13 µM, respectively). It decreases disease severity in a mouse model of collagen-induced arthritis when administered at doses ranging from 0.8 to 20 mg/kg. GW 856553X (1.2 and 12 mg/kg) improves survival, normalizes blood pressure, and reduces increases in plasma levels of HDL, LDL, and triglycerides in spontaneously hypertensive stroke-prone rats fed a high-salt high-fat diet.Formal Name: 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-3-pyridinecarboxamide. CAS Number: 585543-15-3. Synonyms: GSK-AHAB, Losmapimod, SB 856553. Molecular Formula: C22H26FN3O2. Formula Weight: 383.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS (pH7.2)(1:50): 0.01 mg/mL, PBS (pH 7.2): insolub,e. lambdamax: 233 nm. SMILES: FC1=CC(C(NC2CC2)=O)=CC(C3=CC=C(C(NCC(C)(C)C)=O)C=N3)=C1C. InChi Code: InChI=1S/C22H26FN3O2/c1-13-17(9-15(10-18(13)23)21(28)26-16-6-7-16)19-8-5-14(11-24-19)20(27)25-12-22(2,3)4/h5,8-11,16H,6-7,12H2,1-4H3,(H,25,27)(H,26,28). InChi Key: KKYABQBFGDZVNQ-UHFFFAOYSA-N.