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  2. Immunology/Inflammation
  3. COX
  4. NS-398

NS-398 是一種非甾體類抗炎劑，具有解熱作用，可用于緩解疼痛的研究。NS-398 能夠選擇性地抑制 COX-2 的活性，IC50 值為 3.8 μM，在 100 μM 的濃度下，對 COX-1 的活性沒有作用。

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NS-398 Chemical Structure

NS-398 Chemical Structure

CAS No. : 123653-11-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
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1 mg ￥250
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5 mg ￥500
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10 mg ￥700
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25 mg ￥1400
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50 mg ￥2260
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100 mg ￥3500
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Customer Review

    NS-398 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    Expression of NF?κB p65 protein is regulated by COX?2. MG?63 cells were infected with control or COX?2?overexpressing lentivirus, and treated with or without the COX?2 inhibitor NS398 or the PI3K inhibitor LY294002. (A)The expression of NF-κB p65 (green) in each group was determined by immunofluorescence. (B) Quantification of NF-κB p65 expression.

    NS-398 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    Expression of E-cadherin and vimentin is regulated by COX?2. MG?63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX?2 inhibitor NS398 or the PI3K inhibitor LY294002. (A) The expression of E-cadherin (green) in each group was determined using immunofluorescence. (B) Quantification of E?cadherin expression.

    NS-398 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    Expression of E-cadherin and vimentin is regulated by COX?2. MG?63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX?2 inhibitor NS398 or the PI3K inhibitor LY294002. (C) The expression of vimentin in each group. (D) Quantification of vimentin expression.

    查看 COX 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.

    IC50 & Target[1]

    COX-2

    3.8 μM (IC50)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    20 μM
    Compound: 1, NS-398
    Inhibition of mPGES-1 in human A549 cell microsomes assessed as conversion of PGH2 into PGE2 at 0 degC after 5 mins by HPLC-UV analysis
    Inhibition of mPGES-1 in human A549 cell microsomes assessed as conversion of PGH2 into PGE2 at 0 degC after 5 mins by HPLC-UV analysis
    		[PMID: 22209272]
    HaCaT IC50
    10 nM
    Compound: NS-398
    Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA
    Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA
    		[PMID: 15387642]
    RAW264.7 IC50
    > 10 μM
    Compound: NS-398
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry
    		[PMID: 11678654]
    RAW264.7 IC50
    0.007 μM
    Compound: NS-398
    Inhibition of mPGES-1 in mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 production after 24 hrs
    Inhibition of mPGES-1 in mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 production after 24 hrs
    		[PMID: 27720548]
    RAW264.7 IC50
    0.007 μM
    Compound: NS-398
    Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay
    Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay
    		[PMID: 24656662]
    RAW264.7 IC50
    0.00723 μM
    Compound: NS-398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production after 24 hrs by enzyme immunoassay
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production after 24 hrs by enzyme immunoassay
    		[PMID: 29107425]
    RAW264.7 IC50
    0.05 μM
    Compound: NS-398
    Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay
    Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay
    		[PMID: 19233646]
    RAW264.7 IC50
    0.1 μM
    Compound: NS-398
    Inhibition of IFN-gamma/LPS-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by EIA method
    Inhibition of IFN-gamma/LPS-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by EIA method
    		[PMID: 25027933]
    RAW264.7 IC50
    0.81 μM
    Compound: NS-398
    Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay
    Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay
    		[PMID: 20056549]
    RAW264.7 IC50
    2.1 μM
    Compound: NS-398
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as PGE2 accumulation after 20 hrs by RIA
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as PGE2 accumulation after 20 hrs by RIA
    		[PMID: 11678654]
    RAW264.7 IC50
    4.8 μM
    Compound: NS-398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production by EIA
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production by EIA
    		[PMID: 20004572]
    RAW264.7 IC50
    6.7 nM
    Compound: NS-398
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    		[PMID: 31747281]
    RAW264.7 IC50
    6.74 μM
    Compound: NS398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
    		[PMID: 28408221]
    RAW264.7 IC50
    63.7 μM
    Compound: NS-398
    Inhibition of COX1 in mouse RAW264.7 cells by enzyme immunoassay
    Inhibition of COX1 in mouse RAW264.7 cells by enzyme immunoassay
    		[PMID: 20056549]
    RAW264.7 IC50
    7 nM
    Compound: NS-398
    Suppression of PGE2 production in LPS-induced mouse RAW264.7 cells after 24 hrs by enzyme immunoassay
    Suppression of PGE2 production in LPS-induced mouse RAW264.7 cells after 24 hrs by enzyme immunoassay
    		[PMID: 26602278]
    RAW264.7 IC50
    7.01 nM
    Compound: NS398
    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
    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
    		[PMID: 24360561]
    RAW264.7 IC50
    7.23 nM
    Compound: NS-398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production pretreated for 1 hr followed by LPS addition measured after 24 hrs
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production pretreated for 1 hr followed by LPS addition measured after 24 hrs
    		[PMID: 29102229]
    SK-BR-3 IC50
    0.68 μM
    Compound: 1
    Inhibition of aromatase in human SKBR3 cells by tritiated water release assay
    Inhibition of aromatase in human SKBR3 cells by tritiated water release assay
    		[PMID: 18271519]
    SK-BR-3 IC50
    0.72 μM
    Compound: 2e
    Cytotoxicity against human SK-BR-3 cells after 24 hrs by MTT assay relative to NS398
    Cytotoxicity against human SK-BR-3 cells after 24 hrs by MTT assay relative to NS398
    		[PMID: 17095221]
    體外研究
    (In Vitro)

    NS-398 是一種非甾體抗炎劑，選擇性抑制前列腺素 G/H 合酶/環(huán)氧合酶 (COX-2) 活性，IC50 為 3.8 μM，在 100 μM 時對 COX-1 沒有影響[1]。NS-398 微弱抑制綿羊精囊微粒體中的 PG 內(nèi)過氧化物合酶活性 (IC50: 11 μM)[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    NS-398 (0.5-10 mg/kg，po) 劑量依賴性地抑制大鼠爪水腫，ED30 為 1.14 mg/kg，顯示出對輔助性關(guān)節(jié)炎的改善作用 (ED 30，4.69 mg/kg)，具有劑量依賴性鎮(zhèn)痛作用 (ED50，1.65 mg/kg)，并在大鼠中具有解熱作用 (ED50，1.84 mg/kg) 。在小鼠中，NS-398 抑制乙酸誘導(dǎo)的扭體反應(yīng)，ED50 為 8.2 mg/kg[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    314.36

    Formula

    C13H18N2O5S
    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 33.33 mg/mL (106.02 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.1811 mL 15.9053 mL 31.8107 mL
    5 mM 0.6362 mL 3.1811 mL 6.3621 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (7.95 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (5.31 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料
    參考文獻
    Animal Administration
    [2]

    Mice[2]
    Briefly, male ddy mice weighing about 30 g are used. The writhing syndrome is induced by injecting 0.75% of acetic acid, intraperitoneally. Ten minutes later, the number of writhings are counted for the next 10 min. NS-398 is administered orally 30 min prior to the injection. The analgesic effect is expressed as % of inhibition, compared with the vehicle-treated control[2].
    Rats[2]
    Briefly, male Lewis rats weighing about 160 g are used. Arthritis is induced by injecting 0.1 mL of 0.7% Mycobacterium tubercu-losis-liquid paraffin into the left hind paw. On day 15, the rats are grouped according to the degree of secondary lesions in the right hind paw. NS-398 is administered orally once daily from days 15 to 18. Foot volume is measured on day 19. Relative edema volume (REV) is calculated for each animal[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1811 mL 15.9053 mL 31.8107 mL 79.5267 mL
    5 mM 0.6362 mL 3.1811 mL 6.3621 mL 15.9053 mL
    10 mM 0.3181 mL 1.5905 mL 3.1811 mL 7.9527 mL
    15 mM 0.2121 mL 1.0604 mL 2.1207 mL 5.3018 mL
    20 mM 0.1591 mL 0.7953 mL 1.5905 mL 3.9763 mL
    25 mM 0.1272 mL 0.6362 mL 1.2724 mL 3.1811 mL
    30 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6509 mL
    40 mM 0.0795 mL 0.3976 mL 0.7953 mL 1.9882 mL
    50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5905 mL
    60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
    80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
    100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產(chǎn)品名稱：
    NS-398
    目錄號：
    HY-13913
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