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Celecoxib. (Synonyms: 塞来昔布; SC 58635)

目录号: PC14044 纯度: ≥98%

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

CAS No. :169590-42-5

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PC14044-100mg	100mg	¥588.00	请登录
PC14044-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥223.00	请登录

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中文名称

Celecoxib.

中文别名

塞来昔布;4-[5-(4-甲基苯基)-3-(三氟甲基)吡挫-1-基]苯磺酰胺;塞来西布;赛利克西;塞来考昔;塞来克西;噻利考西;赛来克西;2-氟-4-甲氧基苯酚;3-甲基-1,3-丁二醇;Celecoxib 塞来昔布;Celocoxib 抑制剂;塞来昔布 EP标准品;塞来昔布 USP标准品;塞来昔布标准品;塞来昔布（塞内昔布）;塞来昔布-D7;塞内昔布;塞内昔布,BR;塞内昔布,塞来考昔中间体;塞內克西;他克莫司;塞来昔布,塞内昔布,赛利克西;4-[5-(4-甲苯基)-3-(三氟甲基)-1H-吡唑-1-基]甲磺酰胺;5-(4-甲苯基)-1-(4-磺酰基苯基)-3-(三氟甲基)吡唑;希乐葆;赛来昔布;塞来昔布，医药级,纯度:>99%

英文名称

Celecoxib

英文别名

Celecoxib;CELEBREX;4-[[5-(4-METHYLPHENYL)-3-TRIFLUOROMETHYL]-1H-PYRAZOL-YL]BENZENESULFONAMIDE;4-[5-((4-METHYLPHENYL)-3-TRIFLUORPMETHYL)-1H-PYRAZOL-YL]BENENESULFONAMIDE;Celecoxib, 4-[5-(4-Methylphenyl)-3-trifluoromethyl)-1H-pyrazol-yl]benzenesulfonamide;Benzenesulfonamide, 4-5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl-;4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide;Celebra-;4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-pyrazol-1-yl]benzenesulfonamide;Celexibn;IPTG;1-(4-sulphamoylphenyl)-3-trifluoromethyl-5-(p-tolyl)-pyrazole;4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide;4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene sulfona;Celebrex,Celebra;Celecox;celexicob;Celocoxib;N-[4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1yl]phenylsulfonyl]benzensulfonamide;YM 177;4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide;CJ-016377;CP-598107;SC-58635;YM-177;5-(4-Methylphenyl)-1-(4-sulfamoylphenyl)-3-(trifluoromethyl)pyrazole;4-[5-(4-Methylphenyl)-3-trifluoromethyl)-1H-pyrazol-yl]benzenesulfonamide;Celebra;SC 58635;Onsenal;YM177;Celecoxibum;SC58635;C17H14F3N3O2S;p-(5-p-Tolyl-3-(trifluoromethyl)pyrazol-1-yl)benzenesulfonamide;4-(5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide;JCX84Q7J1L

Cas No.

169590-42-5

分子式

C₁₇H₁₄F₃N₃O₂S

分子量

381.37

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

产品详情

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

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.

性状

Solid

IC50 & Target[1][2]

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).
Targeting the YAP/TAZ transcriptional target cyclooxygenase 2 (COX-2) using celecoxib inhibits cell proliferation and tumorigenesis in NF2 mutant cells.

Medlife 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. 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. 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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Penning TD, et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). J Med Chem. 1997 [Information]

[2]. Liu DB, et al. Celecoxib induces apoptosis and cell-cycle arrest in nasopharyngeal carcinoma cell lines via inhibition of STAT3 phosphorylation. Acta Pharmacol Sin. 2012 May;33(5):682-90. [Information]

[3]. Suri A, et al. The effect of celecoxib on tumor growth in ovarian cancer cells and a genetically engineered mouse model of serous ovarian cancer. Oncotarget. 2016 Apr 8. [Information]

[4]. Hou XL, et al. Combination of fasudil and celecoxib promotes the recovery of injured spinal cord in rats better than celecoxib or fasudil alone. Neural Regen Res. 2015 Nov;10(11):1836-40. [Information]

[5]. Liu C, et al. Celecoxib alleviates nonalcoholic fatty liver disease by restoring autophagic flux. Sci Rep. 2018 Mar 7;8(1):4108. [Information]

[6]. Pobbati AV, et al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635. [Information]

溶解度数据

体外研究:

DMSO : ≥ 50 mg/mL (131.11 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

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
10 mM	0.2622 mL	1.3111 mL	2.6221 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.56 mM，饱和度未知) 的澄清溶液。
以 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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.56 mM，饱和度未知) 的澄清溶液。
以 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 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玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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