S-2474
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), 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 agent.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 158089-95-3
- 分子式: C20H31NO3S
- 分子量:365.53
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
COX-2 11 nM (IC50) |
COX-1 27 μM (IC50) |
5-LO |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
10 μM
Compound: 10b
|
In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells
In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells
|
[PMID: 10821716] |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 158089-95-3
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分子量 365.53
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分子式 C20H31NO3S
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SMILES
OC1=C(C(C)(C)C)C=C(/C=C2CCN(CC)S\2(=O)=O)C=C1C(C)(C)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
Cell Assay[2]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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. [Content Brief]
[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. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)