|2-(6-(4-氯苯基)-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪-5-基)乙酸|CsnPharm

CAS No.: 156897-06-2

Synonyms: ML-3000

Licofelone is a dual COX/LOX inhibitor being considered as a treatment for osteoarthritis.

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400-920-2911

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400-920-2911

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描述Metabolism of free arachidonic acid (AA), liberated by phospholipase A2 enzymes, leads to the formation of prostanoids and leukotrienes (LTs) that are considered as potent mediators of inflammatory reactions^[3]. Whereas the cyclooxygenases (COXs)-1 and -2 catalyse the initial steps in the biosynthesis of prostanoids, 5-lipoxygenase (5-LOX) is the key enzyme in the generation of LTs. Licofelone (ML-3000) is a dual inhibitor of and cyclooxygenase being considered as a treatment for osteoarthritis. Dog model of osteoarthritis was orally administered with Licofelone twice daily with food, at a total daily dose of 2.5 mg/kg or 5.0 mg/kg for 8 weeks. It was found that Licofelone treatment markedly reduced the level of chondrocyte apoptosis to the same extent in both therapeutic groups, the levels of caspase-3, COX-2, and iNOS in cartilage from both condyles and plateaus were also significantly decreased, compared to the placebo group^[4]. Licofelone at 195 nM to 50 µM for 72 h reversed the stem-like properties of ovarian multicellular tumor spheroids (MCTS). Importantly, the combination of licofelone (50 mg/kg) with paclitaxel (12 mg/kg) prolonged the median survival of ovarian cancer PDX (patient-derived tumor xenograft) mice model (>141 days) relative to paclitaxel (115 days), licofelone (37 days), or vehicle (30 days)^[5].
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CAS号	156897-06-2	储存条件	粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C23H22ClNO2	运输	蓝冰
分子量	379.88	别名	ML-3000

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