Identification | Back Directory | [Name]
Darbufelone mesilate | [CAS]
139340-56-0 | [Synonyms]
CI 1004 CI-1004 mesylate DARBUFELONE MESILATE Darbufelone (mesylate) (5Z)-2-Amino-5-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one methanesulfonate | [Molecular Formula]
C18H24N2O2S.CH4O3S | [MDL Number]
MFCD00906463 | [MOL File]
139340-56-0.mol | [Molecular Weight]
428.57 |
Hazard Information | Back Directory | [Uses]
Anti-inflammatory; antiarthritic (dual cyclooxygenase and 5-lipoxygenase inhibitor). | [in vivo]
Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis[1]. When mice are treated with Darbufelone at dosage of 80 mg/kg/day, the tumor volumes decrease in a time-dependent manner. In contrast, lower dose of Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, the tumor weight in mice treated with Darbufelone (80 mg/kg/day) is reduced by 30.2% in comparison with control group[2]. | [IC 50]
PGF2α; LTB4; PGHS-2: 0.19 μM (IC50); PGHS-1: 20 μM (IC50) |
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