ZLJ-6
目录号 : GC11203Dual inhibitor of cyclooxygenase/5-lipoxygenase
Cas No.:1051931-39-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
Cas No. | 1051931-39-5 | SDF | |
化学名 | (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 | ||
分子式 | C12H13N3O3S • CH3SO3H | 分子量 | 375.4 |
溶解度 | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6638 mL | 13.3191 mL | 26.6383 mL |
5 mM | 0.5328 mL | 2.6638 mL | 5.3277 mL |
10 mM | 0.2664 mL | 1.3319 mL | 2.6638 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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