NS-398 | N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide | COX-2 Inhibitor

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NS-398 98%

货号：A113156 同义名： N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide

NS-398是一种非甾体抗炎剂，具有镇痛和退热作用。它选择性抑制前列腺素G/H合酶2/环氧合酶2（COX-2）的活性，IC50值为3.8 μM，而对COX-1在100 μM时没有影响。

NS-398 化学结构
CAS号：123653-11-2

NS-398 3D分子结构
CAS号：123653-11-2

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NS-398 纯度/质量文件产品仅供科研

货号：A113156 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

环氧化酶亚型比较

产品名称	COX ↓ ↑	COX-1 ↓ ↑	COX-2 ↓ ↑	纯度
Piroxicam	✔			98%
Salicylic acid	✔			98%
Phenacetin	✔			98%
Etodolac	✔			99%
Flunixin meglumine	✔			98%
Ibuprofen L-lysine	✔			99%
Nabumetone	✔			98%
Acemetacin	✔			98%
Diflunisal	✔			98%
Pranoprofen	✔			98%
Ampiroxicam	✔			98%
Meloxicam	✔			98%
Sulindac	✔			98%
Ketoprofen		✔		98%
Mefenamic Acid		✔		95%
Bromfenac sodium		✔		98%
Oxaprozin		✔		99%
Aspirin		✔		99%
Nepafenac		✔		98%
Zaltoprofen		✔		99%
Salicin		✔		98%
Suprofen		✔		99%+
Xanthohumol		✔		99%
Parecoxib			✔	98%
Tolfenamic Acid			+++ COX-2, IC50: 0.2 μM	98%
Etoricoxib			✔	99%
Niflumic Acid			✔	98%
Valdecoxib			++++ COX-2, IC50: 5 nM	99+%
Ibuprofen		+ COX-1, IC50: 13 μM	+ COX-2, IC50: 370 μM	98%
Indomethacin		++ COX1, IC50: 0.28 μM	+ COX-2, IC50: 14 μM	97%
Lornoxicam		++++ COX-1, IC50: 5 nM	++++ COX-2, IC50: 8 nM	98%
Meclofenamic acid sodium		++++ COX-1, IC50: 40 nM	+++ COX-2, IC50: 50 nM	99%
Rofecoxib			++++ COX-2, IC50: 18 nM	98%
Asaraldehyde			✔	98%
Naproxen		+ COX-1, IC50: 8.7 μM	+ COX-2, IC50: 5.2 μM	98%
Diclofenac Sodium Salt		+++ COX-1, IC50: 60 nM	+++ COX-2, IC50: 200 nM	98%
NS-398			++ COX-2, IC50: 3.8 μM	98%
Amfenac Sodium Hydrate		++ COX-1, IC50: 250 nM	+++ COX-2, IC50: 150 nM	98%+
Nimesulide			+ COX-2, IC50: 26 μM	98%
Lumiracoxib		++ COX-1, Ki: 3 μM	+++ COX-2, Ki: 60 nM	98%
Rutaecarpine			✔	95%
Celecoxib			++++ COX-2, IC50: 40 nM	98%
Carprofen			++++ canine COX2, IC50: 30 nM	98%
Ketorolac		++ COX-1 (human), IC50: 1.23 μM	++ COX-2 (human), IC50: 3.50 μM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

NS-398 生物活性

靶点

COX-2

COX-2, IC50:3.8 μM

描述

NS-398 is a novel anti-inflammatory and analgesic agent. The COX-1 activity was completely unaffected by 100μ M NS-398, whereas the COX-2 activity was concentration-dependently inhibited with IC50 of 3.8μ M^[3]. NS-398 shows the anti-inflammatory and analgesic effects with the effective dose range being 0.3∼5 mg/kg in rats^[4].In vitro experiments, NS-398 inhibited the proliferation and maturation of differentiated myogenic precursor cells, which suggested a detrimental effect on skeletal muscle healing. In the NS-398-treated mice, muscle regeneration delayed at early time points after injury^[5].NS-398 decreased the regeneration of injured muscle by delaying the maturation of regenerating myofibers, and promoted fibrosis by up-regulating TGF-β1 expression. NS-398 administration also reduced the inflammatory response and up-regulated myostatin expression^[5]. NS-398 (10 mM) can induce apoptosis in LNCaP cells^[6]. When treated with NS-398, the C4-2b cells were observed to continue to proliferate and continued to retain malignant phenotype characteristics. NS-398 treatment resulted in C4-2b cell differentiation into an unusual neuroendocrine-like cell which produced both epithelial and neuronal proteins. Moreover, this C4-2b cellular response to NS-398 was mediated by NF-kappa beta transcription factor activation^[6]. Cox-2 is involved in the pathogenesis of Noise-induced hearing loss (NIHL), and pre-treatment with the Cox-2 inhibitor NS398 could inhibit Cox-2 expression during noise overstimulation attenuating noise-induced hearing loss and hair cell damage^[7].

NS-398 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HaCaT cells		Function assay	24 h	Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA, IC50=0.01 μM	15387642
HUVEC		Function assay	18 h	Antiangiogenic activity against VEGFA-stimulated capillary differentiation in HUVEC after 18 hrs by matrigel assay	23110475
HUVEC		Function assay	48 h	Antiangiogenic activity against VEGFA-stimulated cell proliferation in HUVEC after 48 hrs by BrdU incorporation assay	23110475
K562 cells		Function assay	4 days	Inhibition of COX2 in human K562 cells assessed as blockade of AML1-ETO protein-dependent erythroid differentiation after 4 days by benzidine staining method	19172146

NS-398 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00172627	-		Unknown	-	Taiwan ... 展开 >> Shih-Pei Huang Recruiting Taipei, Taiwan Contact: Shih-Pei Huang, MD 886-2-23123456 ext 3353 dtmeda5@ha.mc.ntu.edu.tw 收起 <<

NS-398 参考文献

[1]Sun Y, Yu J, et al. Inhibition of cyclooxygenase-2 by NS398 attenuates noise-induced hearing loss in mice. Sci Rep. 2016 Mar 3;6:22573.

[2]Meyer-Siegler K. COX-2 specific inhibitor, NS-398, increases macrophage migration inhibitory factor expression and induces neuroendocrine differentiation in C4-2b prostate cancer cells. Mol Med. 2001 Dec;7(12):850-60.

[3]Kava MS, Blue DR Jr, Vimont RL, Clarke DE, Ford AP. Alpha1L-adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man. Br J Pharmacol. 1998 Apr;123(7):1359-66. doi: 10.1038/sj.bjp.0701748. PMID: 9579731; PMCID: PMC1565303.

[4]Futaki N, Takahashi S, Yokoyama M, Arai I, Higuchi S, Otomo S. NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro. Prostaglandins. 1994 Jan;47(1):55-9. doi: 10.1016/0090-6980(94)90074-4. PMID: 8140262.

[5]Shen W, Li Y, Tang Y, Cummins J, Huard J. NS-398, a cyclooxygenase-2-specific inhibitor, delays skeletal muscle healing by decreasing regeneration and promoting fibrosis. Am J Pathol. 2005 Oct;167(4):1105-17. doi: 10.1016/S0002-9440(10)61199-6. PMID: 16192645; PMCID: PMC1603662.

[6] Meyer-Siegler K. COX-2 specific inhibitor, NS-398, increases macrophage migration inhibitory factor expression and induces neuroendocrine differentiation in C4-2b prostate cancer cells. Mol Med. 2001 Dec;7(12):850-60. PMID: 11876163; PMCID: PMC1950011.

[7]Sun Y, Yu J, Lin X, Tang W. Inhibition of cyclooxygenase-2 by NS398 attenuates noise-induced hearing loss in mice. Sci Rep. 2016 Mar 3;6:22573. doi: 10.1038/srep22573. PMID: 26934825; PMCID: PMC4776277.

NS-398 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.91mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL

NS-398 技术信息

CAS号	123653-11-2
分子式	C₁₃H₁₈N₂O₅S
分子量	314.357

别名	N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(111.34 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

HaCaT cells		Function assay	24 h	Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA, IC50=0.01 μM	15387642
HUVEC		Function assay	18 h	Antiangiogenic activity against VEGFA-stimulated capillary differentiation in HUVEC after 18 hrs by matrigel assay	23110475
HUVEC		Function assay	48 h	Antiangiogenic activity against VEGFA-stimulated cell proliferation in HUVEC after 48 hrs by BrdU incorporation assay	23110475
K562 cells		Function assay	4 days	Inhibition of COX2 in human K562 cells assessed as blockade of AML1-ETO protein-dependent erythroid differentiation after 4 days by benzidine staining method	19172146
MDA-MB-231 cell		Function assay		Reduction in PGE2 levels in MDA-MB-231 cell	16480277
PMA-Ion-stimulated human PBL	5 μM	Function assay	20 h	Inhibition of COX2 expression in PMA-Ion-stimulated human PBL at 5 uM after 20 hrs by Western blot analysis	23047231
RAW264.7 cells		Function assay		Evaluated for inhibition of COX-2 catalyzed PGE-2 production from LPS induced RAW 264.7 cells, IC50=0.5 μM	14980657
RAW264.7 cells		Function assay		Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production by EIA, IC50=4.8 μM	20004572
RAW264.7 cells		Function assay	24 h	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA, IC50=0.00701 μM	24360561
RAW264.7 cells		Function assay		Inhibition of PGE2 production in LPS-induced mouse RAW264.7 cells, IC50=0.007 μM	25453800
RAW264.7 cells		Function assay	17-20 h	Inhibition of IFN-gamma/LPS-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by EIA method, IC50=0.1 μM	25027933
RAW264.7 cells		Function assay		Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay, IC50=0.05 μM	19233646
RAW264.7 cells		Function assay		Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay, IC50=0.81 μM	20056549
SKBr3 cells		Function assay	24 h	Reduction in CYP19 mRNA expression in SKBr3 cells after 24h exposure to 25uM relative to control	16480277
SKBR3 cells		Function assay		Inhibition of aromatase in human SKBR3 cells by tritiated water release assay, IC50=0.68 μM	18271519
SK-BR-3 cells		Cytotoxicity assay	24 h	Cytotoxicity against human SK-BR-3 cells after 24 hrs by MTT assay relative to NS398, IC50=0.72 μM	17095221
SK-BR-3 cells		Function assay		Inhibition of CYP450 aromatase activity in SK-BR-3 cells, IC50=0.68 μM	16480277

NS-398 98%

NS-398 纯度/质量文件产品仅供科研

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NS-398 98%

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全球学术期刊中引用的产品

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NS-398 生物活性

NS-398 细胞研究

NS-398 临床研究

NS-398 参考文献

NS-398 实验方案

NS-398 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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临床研究

确认信息

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