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  • ZLJ-6
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ZLJ-6

Dual inhibitor of cyclooxygenase/5-lipoxygenase

原价
¥650-11175
价格
520-8940
ZLJ-6的二维码

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  • 货号: ajci6648
  • CAS: 1051931-39-5
  • 别名:
  • 分子式: C12H13N3O3S ? CH3SO3H
  • 分子量: 375.4
  • 纯度: >98%
  • 溶解度: ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide
  • 储存: Store at -20°C
  • 库存: 现货

Background

IC50: 0.73, 0.31, and 0.99 μM for COX-1, COX-2, and 5-LO, respectively


ZLJ-6 is a dual inhibitor of COX and 5-lipoxygenase (5-LO).


Cyclooxygenase (COX) is an enzyme that is responsible for formation of prostanoids, such as thromboxane and prostaglandins such as prostacyclin. 5-lipoxygenase (5-LO) is the major source of leukotrienes.


In vitro: ZLJ-6 was identified as a potent inhibitor of cyclooxygenase in human whole blood. It also inhibited the production of thromboxane B(2) and prostaglandin E(2) in calcium ionophore A23187-induced human and rat whole blood, and rat peritoneal leukocytes. ZLJ-6 suppressed the activity of 5-lipoxygenase in the rat basophilic leukemia (RBL-1) cell lysate and in intact cells and reduced the generation of leukotriene B(4) (LTB(4)) in A23187-stimulated human or rat whole blood, and rat peritoneal leukocytes [1].


In vivo: Orally administered ZLJ-6 demonstrated potent anti-inflammatory activity in the carrageenin-induced paw oedema model in rats and showed analgesic activity in the acetic acid-induced abdominal construction model in mice. No gastrointestinal ulcers were found with the anti-inflammatory dose (30 mg/kg) in normal rats [1].


Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Li, L.?,Ji, H.,Sheng, L., et al. The anti-inflammatory effects of ZLJ-6, a novel dual cyclooxygenase/5-lipoxygenase inhibitor. European Journal of Pharmacology 607 (1-3), 244-250 (2009).

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