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RPR-200765A RPR-200765A is a potent and selective inhibitor of p38 MAP kinase (IC50 = 50 nM). It inhibits LPS-stimulated TNFalpha release both in vitro, from human monocytes (EC50 = 110 nM), and in vivo in Balb/c mice (ED50 = 6 mg/kg). At oral doses between 10 and 30 mg/kg/day it reduces the incidence and progression in the rat streptococcal cell wall (SCW) arthritis model when administered in either prophylactic or therapeutic dosing regimens. The compound, which is a mesylate salt and exists as a stable monohydrate, shows good oral bioavailabiltiy (F = 50% in the rat) and excellent chemical stability. The data from the SCW disease model suggests that RPR200765A could exhibit a profile of disease modifying activity in rheumatoid arthritis (RA) patients which is not observed with current drug therapies. Synonyms: RPR-200765; RPR200765; RPR 200765; RPR-200765A. CAS No. 218158-45-3. Molecular formula: C24H25FN4O4. Mole weight: 452.48. BOC Sciences 11
RPR-200765A Mesylayte RPR-200765A Mesylayte, a potent and selective inhibitor of p38 MAP kinase (IC50 = 50 nM), could exhibit a profile of disease modifying activity in rheumatoid arthritis (RA) patients which is not observed with current drug therapies. RPR-200765A inhibits LPS-stimulated TNFalpha release both in vitro, from human monocytes (EC50 = 110 nM), and in vivo in Balb/c mice (ED50 = 6 mg/kg). Synonyms: [2-[4-(4-fluorophenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-5-methyl-1,3-dioxan-5-yl]-morpholin-4-ylmethanone; RPR 200765A; RPR-200765 A; 218158-45-3 (RPR-200765, free base). Grades: >98%. CAS No. 218162-38-0. Molecular formula: C24H25FN4O4. Mole weight: 452.48. BOC Sciences 10

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