WAY-196025
WAY-196025 is a selective and orally active indole cytosolic phospholipase A2 alpha (cPLA2α) inhibitor with an IC50 of 0.01μM and a Kd of 0.013 μM. WAY-196025 can inhibit the production of prostaglandins (such as PGE2) and leukotrienes (such as LTB4), and reduce the release of inflammatory mediators. WAY-196025 can be used for the researches of inflammation and immunology, such as asthma.
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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: 540523-42-0
- 分子式: C42H41ClN2O4S
- 分子量:705.30
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Phospholipase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
cPLA2α 0.01 μM (IC50) |
cPLA2α 0.013 μM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MC9 | IC50 |
>1 μM
Compound: 121
|
Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells
Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells
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[PMID: 18498150] |
| MC9 | IC50 |
0.006 μM
Compound: 121
|
Inhibition of PGF2alpha production in mouse MC9 cells
Inhibition of PGF2alpha production in mouse MC9 cells
|
[PMID: 18498150] |
| MC9 | IC50 |
0.012 μM
Compound: 121
|
Inhibition of LTB4 production in mouse MC9 cells
Inhibition of LTB4 production in mouse MC9 cells
|
[PMID: 18498150] |
化学情報
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CAS 番号 540523-42-0
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分子量 705.30
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分子式 C42H41ClN2O4S
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SMILES
O=C(O)C1=CC=C(CCCC2=C(CCNS(=O)(CC3=C(C)C=CC=C3C)=O)N(C(C4=CC=CC=C4)C5=CC=CC=C5)C6=C2C=C(Cl)C=C6)C=C1
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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
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
純度とドキュメンテーション
参考文献
[1]. McKew JC, et al. Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib. J Med Chem. 2008 Jun 26;51(12):3388-413. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)