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Submit ReviewNS 398 is a selective cyclooxygenase-2 inhibitor (IC50 values are 3.8 and > 100 μM for COX-2 and COX-1 respectively). Induces apoptosis in colorectal tumor cells and elevates COX-2 protein expression in vitro. Orally active and non-ulcerogenic analgesic and anti-inflammatory in vivo.
NS 398 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 314.36 |
公式 | C13H18N2O5S |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 123653-11-2 |
PubChem ID | 4553 |
InChI Key | KTDZCOWXCWUPEO-UHFFFAOYSA-N |
Smiles | CS(=O)(=O)NC1=C(OC2CCCCC2)C=C(C=C1)[N+]([O-])=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 31.44 | 100 |
以下数据基于产品分子量 314.36。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.18 mL | 15.91 mL | 31.81 mL |
5 mM | 0.64 mL | 3.18 mL | 6.36 mL |
10 mM | 0.32 mL | 1.59 mL | 3.18 mL |
50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
参考文献是支持产品生物活性的出版物。
Elder et al (2002) The MEK/ERK pathway mediates COX-2-selective NSAID-induced apoptosis and induced COX-2 protein expression in colorectal carcinoma cells. Int.J.Cancer 99 323 PMID: 11992399
Futaki et al (1993) NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimal stomach lesions. Gen.Pharmacol. 24 105 PMID: 8482483
Futaki et al (1994) NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro. Prostaglandins 47 55 PMID: 8140262
If you know of a relevant reference for NS 398, please let us know.
关键词: NS 398, NS 398 supplier, Cyclooxygenase, COX-2, inhibitors, inhibits, COX, Oxygenases, Oxidases, NS398, 0942, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NS 398 的部分引用包括:
Bonfill-Teixidor et al (2017) Differential expression of E-type prostanoid receptors 2 and 4 in microglia stimulated with lipopolysaccharide. J Neuroinflammation 14 3 PMID: 28086956
Bourquin et al (2011) Systemic cancer therapy with a small molecule agonist of toll-like receptor 7 can be improved by circumventing TLR tolerance. Cancer Res 71 5123 PMID: 21697281
Chia et al (2011) Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice. BMC Pharmacol 11 10 PMID: 21955547
Sugiyama et al (2013) The cyclooxygenase-2 selective inhibitor NS-398 does not influence trabecular or cortical bone gain resulting from repeated mechanical loading in female mice. Osteoporos Int 24 383 PMID: 22349912
Wong et al (2009) Cyclooxygenase-2-derived prostaglandin F2alpha mediates endothelium-dependent contractions in the aortae of hamsters with increased impact during aging. Circ Res 104 228 PMID: 19096033
Messerschmidt et al (2019) Osmotic induction of cyclooxygenase-2 in RPE cells: Stimulation of inflammasome activation. Mol Vis 25 329 PMID: 31341381
Wei et al (2015) Proinflammatory cytokines upregulate sympathoexcitatory mechanisms in the subfornical organ of the rat. Hypertension 65 1126 PMID: 25776070
Font-Nieves et al (2012) Induction of COX-2 enzyme and down-regulation of COX-1 expression by lipopolysaccharide (LPS) control prostaglandin E2 production in astrocytes. J Biol Chem 287 6454 PMID: 22219191
Ho et al (2015) Peripheral inflammation increases seizure susceptibility via the induction of neuroinflammation and oxidative stress in the hippocampus. J Virol 22 46 PMID: 26100815
Tunaru et al (2016) Arachidonic acid metabolite 19(S)-HETE induces vasorelaxation and platelet inhibition by activating prostacyclin(IP) receptor. PLoS One 11 e0163633 PMID: 27662627
Liu et al (2014) Uncoupling protein-2 mediates DPP-4 inhibitor-induced restoration of endothelial function in hypertension through reducing oxidative stress. Antioxid Redox Signal 21 1571 PMID: 24328731
Buenestado et al (2012) Roflumilast inhibits the release of chemokines and TNF-α from human lung macrophages stimulated with lipopolysaccharide. Br J Pharmacol 165 1877 PMID: 21913898
Sunters et al (2010) Mechano-transduction in osteoblastic cells involves strain-regulated estrogen receptor alpha-mediated control of Ins-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 receptor-i J Biol Chem 285 8743 PMID: 20042609
Ray et al (2004) Cyclooxygenase-1 and -2 are required for production of infectious pseudorabies virus. PLoS One 78 12964 PMID: 15542648
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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.