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- Cyclooxygenase (COX)
- S-2474
S-2474
S-2474是COX-2和5-lipoxygenase的抑制剂，在人完整的细胞中，对COX-2和COX-1的IC50值分别为11nM和27μM，为一种非甾体抗炎药。
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包装价格促销价数量
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1mg￥8350.006680.00- +
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5mg￥16525.0013220.00- +
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10mg￥28075.0022460.00- +
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20mg￥49587.0039670.00- +
- 货号: ajce47912
- CAS: 158089-95-3
- 别名:
- 分子式: C20H31NO3S
- 分子量: 365.53
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1[1]. S-2474 prevents neurons from Aβ-induced cell death significantly in a concentration-dependent manner (IC50 =26±12 nM). S-2474 (10 μM) completely inhibits Aβ(25-35)-induced neuronal cell death. S-2474 also shows neuroprotective effects in the Aβ(1-40)-induced neuronal cell death. S-2474 inhibits the PGD2 generation in a concentration dependent manner (IC50=69.8±21.9 nM). S-2474 (10 μM) lowers the elevated level of PGD2 significantly and reduces radicals from Aβ(25-35)-treated neurons[2]. S-2474 significantly prevents neurons from undergoing sPLA2-IIA-induced cell death. S-2474 completely ameliorates sPLA2-IIA-induced apoptotic features such as the condensation of chromatin and the fragmentation of DNA. Moreover, S-2474 significantly inhibits the sPLA2-IIA-induced generation of PGD2. S-2474 inhibits sPLA2-IIA-induced neuronal cell death in a concentration-dependent manner (IC50 = 94 nM)[3].
[1]. Yagami T, et al. Effects of S-2474, a novel nonsteroidal anti-inflammatory drug, on amyloid beta protein-induced neuronal cell death. Br J Pharmacol. 2001 Oct;134(3):673-81. [2]. Yagami T, et al. S-2474, a novel nonsteroidal anti-inflammatory drug, rescues cortical neurons from human group IIA secretory phospholipase A(2)-induced apoptosis. Neuropharmacology. 2005 Aug;49(2):174-84. Epub 2005 Apr 1.
Protocol
Cell experiment: | Experiments are principally performed in the two conditions as follows. (i) Neurons (2.5×105 cells/cm2) are treated with 10?μM Aβ(25-35) or Aβ(1-40) in the presence or absence of S-2474 at 37°C. Vehicle controls are treated with culture medium containing 1% deionized water and 0.1% DMSO. Aβ controls are treated with culture medium containing 10?μM Aβ(25-35) and 0.1% DMSO. (ii) Neurons (2.5×105 cells/cm2) are treated with eicosanoids at 37°C. Vehicle controls are treated with culture medium containing 0.1% ethanol. Two different methods are employed for assessment of neurotoxicity of Aβ. First, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide dye (MTT) reduction assay reflecting mitochondrial succinate dehydrogenase activity is employed. Second, residual cells are counted according to morphologic criteria; neurons with intact neurites and a smooth, round soma are considered viable, whereas those with degenerated neurites and an irregular soma are considered nonviable. |
参考文献: [1]. Yagami T, et al. Effects of S-2474, a novel nonsteroidal anti-inflammatory drug, on amyloid beta protein-induced neuronal cell death. Br J Pharmacol. 2001 Oct;134(3):673-81. | |
