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  1. Immunology/Inflammation
  2. COX
  3. Celecoxib

Celecoxib  (Synonyms: 塞來(lái)昔布; SC 58635)

目錄號(hào): HY-14398 純度: 99.09%
COA 產(chǎn)品使用指南

Celecoxib 是一種選擇性的 COX-2 抑制劑,IC50 為 40 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Celecoxib Chemical Structure

Celecoxib Chemical Structure

CAS No. : 169590-42-5

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10 mM * 1 mL in DMSO ¥715
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100 mg ¥650
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1 g ¥2200
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Customer Review

Other Forms of Celecoxib:

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

WB

    Celecoxib purchased from MCE. Usage Cited in: Br J Cancer. 2018 Jan;118(2):213-223.  [Abstract]

    Western blotting of EP2, EP4, COX-2, and PTEN using proteins extracted from SVHUC cells without MCA exposure and MCA-exposed SVHUC cells subsequently cultured for 6 weeks with ethanol or Celecoxib (1 mM). GAPDH served as a loading control.

    Celecoxib purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.  [Abstract]

    L02 cells exposed to PA (200 μM) with different concentrations of Celecoxib (Cel, 5-40 μM) for 24 h. Celecoxib decreases protein expression of COX-2 compared with control as indicated by western blot.

    Celecoxib purchased from MCE. Usage Cited in: Oncol Rep. 2018 Oct;40(4):2242-2250.  [Abstract]

    Effects of Gefitinib(G) and Celecoxib(Cel) on ABCB1 (MDR1), FOXM1 and Bcl 2 protein levels in PC3/DR and DU145/DR cell lines. The effects of Gefitinib, Celecoxib and their combination on ABCB1 (MDR1), FOXM1 and Bcl 2 expression in the PC3/DR and DU145/DR cell lines are determined by a western blot assay.

    查看 COX 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.

    IC50 & Target[1]

    COX-2

    40 nM (IC50)

    COX-1

    15 μM (IC50)

    體外研究
    (In Vitro)

    The selective cyclooxygenase-2 (COX-2) inhibitor Celecoxib (10-75 μM) inhibits the proliferation of the NPC cell lines in a dose-dependent manner. Celecoxib (25 and 50 μM) induces apoptosis and cell-cycle arrest at the G0/G1 checkpoint in the NPC cell lines, which is associated with significantly reduced STAT3 phosphorylation. The genes downstream of STAT3 (ie, Survivin, Mcl-1, Bcl-2 and Cyclin D1) are significantly down-regulated after exposure to Celecoxib (25 and 50 μM)[2].
    Targeting the YAP/TAZ transcriptional target cyclooxygenase 2 (COX-2) using celecoxib inhibits cell proliferation and tumorigenesis in NF2 mutant cells[6].

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

    體內(nèi)研究
    (In Vivo)

    Celecoxib demonstrates potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay with an ED50 of 7.1 mg/kg and reduces chronic inflammation in the adjuvant arthritis model with an ED50 of 0.37 mg/kg/day. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with an ED50 of 34.5 mg/kg. Celecoxib has potency equivalent to that of standard nonsteroidal anti-inflammatory drugs (NSAIDs), yet shows no acute GI toxicity in rats at doses up to 200 mg/kg. In addition, it displays no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days[1]. In the KpB mice fed a high fat diet (obese) and treated with Celecoxib, tumor weight decreases by 66% when compare with control animals. Among KpB mice fed a low fat diet (non-obese), tumor weight decreases by 46% after treatment with Celecoxib[3]. Rat models are orally administrated with Celecoxib (20 mg/kg) and/or intramuscularly with Fasudil (10 mg/kg) for 2 weeks. Results demonstrates that the combined use of Celecoxib and fasudil significantly decreases COX-2 and Rho kinase II expression surrounding the lesion site in rats with spinal cord injury, improves the pathomorphology of the injured spinal cord, and promoted the recovery of motor function[4].

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

    Clinical Trial
    分子量

    381.37

    Formula

    C17H14F3N3O2S

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    塞來(lái)昔布

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : ≥ 50 mg/mL (131.11 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.6221 mL 13.1106 mL 26.2213 mL
    5 mM 0.5244 mL 2.6221 mL 5.2443 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲(chǔ)備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn):

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.56 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (6.56 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

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

      20% SBE-β-CD in Saline 的配制(4°C,儲(chǔ)存一周):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。
    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(guò) 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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(xiàn)
    Cell Assay
    [2]

    The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 h. The cells are then treated with increasing concentrations of Celecoxib (0, 5, 10, 25, 50 or 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 h. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37°C for 4 h. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The percentage growth inhibition is calculated as (ODcontrol?ODdrug)/ODcontrol×100%. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times[2].

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

    Animal Administration
    [3][4]

    Mice[3]
    The KpB mice are monitored weekly by palpation for tumor growth. Celecoxib and placebo treatment is initiated after palpation of a 1 cm tumor in mice on the HFD (obese group) and LFD (non-obese group) (N=15 mice per group). Celecoxib is dissolved in DMSO at 5 mg/mL, further diluted 10 times in 0.5% methylcellulose with 0.025% Tween 80 and injected (IP) daily at a dose of 5 mg/kg body weight for 4 weeks. The tumor sizes are measured once a week by palpation. Tumor volume is calculated using the following equation: volume (mm3)=a×b2/2, where is the largest diameter and b is the smallest diameter. The animals are weighed weekly throughout the study. At sacrifice, mice are weighed and blood samples are taken. Half of the ovarian tumor is snap-frozen and stored at ?80°C, and the other half is fixed in 10% neutral-buffered formalin and paraffin embedded. Mouse heart, lungs and kidneys are also harvested, fixed in formalin and grossly examined for any suspicious lesions before paraffin embedding.
    Rats[4]
    Forty adult, clean, female, Sprague-Dawley rats aged 3 months and weighing 280-330 g, are used. Forty rats are randomized to five groups as follows: sham surgery, model, Celecoxib, fasudil and combination groups, with eight rats in each group. Rats in the Celecoxib group are intragastrically administrated with a suspension of Celecoxib (20 mg/kg), and a suspension of Celecoxib containing 0.5% sodium carboxymethylcellulose is made from the capsules. Rats in the fasudil group are intramuscularly administrated with fasudil hydrochloride injection (10 mg/kg) via the dorsal muscle. Rats in the combination group are administrated with both a suspension of Celecoxib (20 mg/kg) and fasudil hydrochloride (10 mg/kg). The fasudil and Celecoxib doses are based on doses administered to adults and these are adjusted in a pre-study. Administration is once every day for 2 weeks. Subsequently, all rats are treated normally for another 2 weeks, and then sacrificed either for histological examination or for western blot assay.

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

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 2.6221 mL 13.1106 mL 26.2213 mL 65.5531 mL
    5 mM 0.5244 mL 2.6221 mL 5.2443 mL 13.1106 mL
    10 mM 0.2622 mL 1.3111 mL 2.6221 mL 6.5553 mL
    15 mM 0.1748 mL 0.8740 mL 1.7481 mL 4.3702 mL
    20 mM 0.1311 mL 0.6555 mL 1.3111 mL 3.2777 mL
    25 mM 0.1049 mL 0.5244 mL 1.0489 mL 2.6221 mL
    30 mM 0.0874 mL 0.4370 mL 0.8740 mL 2.1851 mL
    40 mM 0.0656 mL 0.3278 mL 0.6555 mL 1.6388 mL
    50 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3111 mL
    60 mM 0.0437 mL 0.2185 mL 0.4370 mL 1.0926 mL
    80 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8194 mL
    100 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6555 mL
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    產(chǎn)品名稱:
    Celecoxib
    目錄號(hào):
    HY-14398
    需求量: