NS-398 (NS398)

別名：N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide

製品コード：S8433 純度：99.80%

NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively.

CAS No. 123653-11-2

サイズ	価格(税別)	在庫状況
10mg	JPY 18100	国内在庫あり
50mg	JPY 67900	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（14）

カスタマーフィードバック1个实验数据

製品安全説明書

現在のバッチを見る：純度： 99.80%

99.80

NS-398 (NS398)関連製品

関連ターゲット	COX-1 COX-2	もっと見る
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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

COXシグナル伝達経路

COX阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
PMA-Ion-stimulated human PBL	Function assay	5 μM	20 h	Inhibition of COX2 expression in PMA-Ion-stimulated human PBL at 5 uM after 20 hrs by Western blot analysis	23047231
SKBr3 cells	Function assay		24 h	Reduction in CYP19 mRNA expression in SKBr3 cells after 24h exposure to 25uM relative to control	16480277
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
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
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
HaCaT cells	Function assay		24 h	Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA, IC50=0.01 μM	15387642
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
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
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
MDA-MB-231 cell	Function assay			Reduction in PGE2 levels in MDA-MB-231 cell	16480277
SKBR3 cells	Function assay			Inhibition of aromatase in human SKBR3 cells by tritiated water release assay, IC50=0.68 μM	18271519
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			Inhibition of PGE2 production in LPS-induced mouse RAW264.7 cells, IC50=0.007 μM	25453800
SK-BR-3 cells	Function assay			Inhibition of CYP450 aromatase activity in SK-BR-3 cells, IC50=0.68 μM	16480277
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

COX-2 ^[1]
(Cell-free assay)

3.8 μM

In Vitro
In vitro	NS-398 inhibits COX-2 enzyme activity in a concentration dependent manner, the IC50 being 3.8 μM, whereas NS-398 at 100μM has no effect on COX-1 activity^[1]. At 10 μM, NS-398 treatment results in increased production of COX-2 and the pro-inflammatory cytokine. NS-398 (10 μM) induces apoptosis in LNCaP cells, but not in the more aggressive, androgen-unresponsive C4-2b cells. The C4-2b cells are observed to continue to proliferate when treated with NS-398 and continues to retain malignant phenotype characteristics. NS-398 treatment results in C4-2b cell differentiation into an unusual neuroendocrinelike cell. These neuroendocrine-like cells produces both epithelial (cytokeratin 18 and prostate specific antigen) and neuronal (neuron-specific enolase and chromogranin A) proteins. Furthermore, this C4-2b cellular response to NS-398 is mediated by NF-kB transcription factor activation. NS-398 induces NF-kB and down-regulates Ikβ-α protein expression in LNCaP C4-2b cells^[2].
細胞実験	細胞株	human prostate carcinoma cell line LNCaP and the LNCaP subline C4-2b
	濃度	10 μM
	反応時間	24, 48, 72 h
	実験の流れ	1×10_⁶ cells are plated in six well cluster plates with 2 ml of medium for 24 h. At time point 0, medium was removed, cells were carefully washed with phosphate buffered saline (PBS) and serum free(SF), phenol-red free medium containing 0.5 μg/ml BSA was added. Incubations are continued for an additional 72 h with or without increasing NS-398 concentrations. NS-398 stocks (5 mM) are dissolved in 0.1% dimethylsulfoxide (DMSO). Cells and culture medium are harvested at 24 h time intervals. Dead cells are removed by gentle washing with PBS and cell number determined by direct counting using trypan blue dye exclusion to identify viable cells. DMSO (0.1%) is added to control cultures.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	c-Myc p-CHK1 / CHK1 LEF1 / active-β-catenin / CXCR4 / Cleaved Caspase 3		31410206
	Growth inhibition assay	Cell viability		30304769

In Vivo
In Vivo	NS398 could inhibit Cox-2 expression induced by acoustic injury and could attenuate noise-induced hearing threshold shifts and cochlear hair cell loss. The inhibition of Cox-2 by NS398 could attenuate Noise-induced hearing loss（NIHL）and related hair cell damage.^[3].
動物実験	動物モデル	CD1 mice
	投与量	20 mg/kg
	投与経路	i.p.

参考
[1] Futaki N, et al. Prostaglandins. 1994, 47(1):55-9. [2] Meyer-Siegler K, et al. Mol Med. 2001, 7(12):850-60. [3] Sun Y, et al. Sci Rep. 2016, 6:22573.

参考

化学情報

分子量	314.36	化学式	C₁₃H₁₈N₂O₅S
CAS No.	123653-11-2	SDF	Download NS-398 (NS398) SDFをダウンロードする
Smiles	CS(=O)(=O)NC1=C(C=C(C=C1)[N+](=O)[O-])OC2CCCCC2
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 62 mg/mL ( (197.22 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):