1. Immunology/Inflammation
  2. COX
  3. Celecoxib

Celecoxib  (Synonyms: 塞来昔布; SC 58635)

目录号: HY-14398 纯度: 99.09%
COA 产品使用指南

Celecoxib 是一种选择性的 COX-2 抑制剂,IC50 为 40 nM。

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Celecoxib Chemical Structure

Celecoxib Chemical Structure

CAS No. : 169590-42-5

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规格 价格 是否有货 数量
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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5 g   询价  
10 g   询价  

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Customer Review

Other Forms of Celecoxib:

MCE 顾客使用本产品发表的 41 篇科研文献

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 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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)

    体外研究
    (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.

    体内研究
    (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 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    塞来昔布

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (131.11 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料
    参考文献
    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.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 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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    • 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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