| CAS NO: | 1051931-39-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 375.4 |
| Cas No. | 1051931-39-5 |
| Formula | C12H13N3O3S·CH3SO3H |
| Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| Chemical Name | (5Z)-2-amino-1,5-dihydro-1-methyl-5-[[4-(methylsulfonyl)phenyl]methylene]-4H-imidazol-4-one, monomethanesulfonate |
| Canonical SMILES | O=S(C1=CC=C(/C=C2C(C)C(N)=NC/2=O)C=C1)(C)=O.CS(=O)(O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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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