LY 178002
目录号 : GC30610LY178002是一种有效的5-lipoxygenase,phospholipaseA2抑制剂,对5-lipoxygenase的IC50值为0.6μM,能够抑制人多形核白细胞产生LTB4,同时可相对较弱地抑制cyclooxygenase的活性。
Cas No.:107889-32-7
Sample solution is provided at 25 µL, 10mM.
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LY 178002 is a potent inhibitor of 5-lipoxygenase, phospholipase A2, with IC50 of 0.6 μM for 5-1ipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
LY178002 inhibits the generation of LTB4, PLA2 and FCO with IC50s of 0.1, 6.3 and 4.2 μM [1].
LY 178002 (50 mg/kg) inhibits soft tissue swelling in the uninjected paw by 81%, and inhibits bone damage in rats. The minimum effective dose for LY178002 is 10 mg/kg p.o. In the established FCA model LY178002 at 50 mg/kg p.o. inhibits the uninjected paw swelling by 75%[1].
[1]. Panetta JA, et al. The anti-inflammatory effects of LY178002 and LY256548. Agents Actions. 1989 Jun;27(3-4):300-2.
Cas No. | 107889-32-7 | SDF | |
Canonical SMILES | O=C1NCS/C1=C/C2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2 | ||
分子式 | C18H25NO2S | 分子量 | 319.46 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.1303 mL | 15.6514 mL | 31.3028 mL |
5 mM | 0.6261 mL | 3.1303 mL | 6.2606 mL |
10 mM | 0.313 mL | 1.5651 mL | 3.1303 mL |
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1. 首先保证母液是澄清的;
2.
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The anti-inflammatory effects of LY178002 and LY256548
LY178002 (5-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene-4-thiazolidinon e) and its N-methyl analog, LY256548, inhibit the enzymatic activity of phospholipase A2, 5-lipoxygenase and fatty acid cycloxygenase. They also inhibit leukotriene B4 production from human polymorphonuclear leukocytes stimulated with the calcium ionophore A23187. Since products of the arachidonic acid cascade have been implicated as important mediators in a variety of inflammatory diseases including arthritis, LY178002 and LY256548 were studied in the Freund's Complete Adjuvant-Induced Arthritis (FCA) model in rats. The compounds were administered orally and inhibition of bone damage and paw swelling was assessed of both the injected and uninjected paws. At 50 mg/kg LY178002 inhibited soft tissue swelling in the uninjected paw by 81% while LY256548 exhibited 57% inhibition. Bone damage was also significantly inhibited by both compounds. A dose response was conducted. The minimum effective dose for LY178002 was 10 mg/kg p.o. In the established FCA model LY178002 at 50 mg/kg p.o. inhibited the uninjected paw swelling by 75% while LY256548 did not show this level of activity. These results suggest that LY178002 and LY256548 may be useful in the treatment of arthritis.
LY178002 reduces rat brain damage after transient global forebrain ischemia
Several feasible mechanisms have been proposed as sources of neuronal damage from ischemia and subsequent reperfusion. Included among these are oxidative damage caused by free radical production and lipid peroxidation and products derived from phospholipid breakdown. A series of 4-thiazolidinone compounds represented by LY178002 (5-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene-4-thiazolidinon e) have been described as inhibitors of multiple enzymes in the arachidonic acid cascade, including fatty acid cyclooxygenase, 5-lipoxygenase, and phospholipase A2. Accordingly, we evaluated LY178002 in a four-vessel occlusion model of global forebrain ischemia with reperfusion. A 2-hour pretreatment of 11 male Wistar rats with 150 mg/kg LY178002 significantly protected against striatal (p = 0.0007) and hippocampal CA1 (p = 0.006) damage after 30 minutes of global ischemia. Similar protection was observed for the striatum (p = 0.005) and hippocampal CA1 layer (p = 0.025) after pretreatment of 13 rats with 50 mg/kg LY178002. We further evaluated LY178002 as a possible inhibitor of lipid peroxidation because part of its chemical structure incorporates the aromatic backbone of the known antioxidant butylated hydroxytoluene. We found LY178002 to be a potent inhibitor of iron-dependent lipid peroxidation. Few substances possessing a single pharmacological activity have been found to be of significant therapeutic benefit in global ischemia of 30 minutes' duration because the mechanisms that lead to cell death in response to ischemia are likely to be multifactorial. Thus, the efficacy of LY178002 in this model may be due to its ability to inhibit multiple sources of damage.