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/ Celecoxib/塞来昔布

Celecoxib/塞来昔布 {[allProObj[0].p_purity_real_show]}

货号：A180379 同义名： 塞来西布 / SC 58635; YM-177

Celecoxib是一种选择性的COX-2抑制剂，IC50值为40 nM。

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Celecoxib/塞来昔布 化学结构 CAS号：169590-42-5
Celecoxib/塞来昔布 化学结构
CAS号：169590-42-5
Celecoxib/塞来昔布 3D分子结构
CAS号：169590-42-5
Celecoxib/塞来昔布 化学结构 CAS号：169590-42-5
Celecoxib/塞来昔布 3D分子结构 CAS号：169590-42-5
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Celecoxib/塞来昔布 纯度/质量文件 产品仅供科研

货号：A180379 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 COX ↓ COX-1 ↓ COX-2 ↓ 其他靶点 纯度
Piroxicam ✔ 98%
Salicylic acid ✔ 98%
Phenacetin ✔ 98%
Etodolac ✔ 99%
Flunixin meglumine ✔ 98%
Ibuprofen L-lysine ✔ 98%
Nabumetone ✔ 98%
Acemetacin ✔ 98%
Diflunisal ✔ 98%
Pranoprofen ✔ 98%
Ampiroxicam ✔ 98%
Meloxicam ✔ 98%
Sulindac ✔ 98%
Ketoprofen ✔ 98%
Mefenamic Acid ✔ 95%
Bromfenac sodium ✔ 98%
Oxaprozin ✔ 99%
Aspirin ✔ 99%
Nepafenac ✔ 98%
Zaltoprofen ✔ 99%
Salicin ✔ 98%
Suprofen ✔ 99%+
Xanthohumol ✔ 99%
Parecoxib ✔ 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

 		98%
Etoricoxib ✔ 99%
Niflumic Acid ✔ 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

 		99+%
Ibuprofen +

COX-1, IC50: 13 μM

 		+

COX-2, IC50: 370 μM

 		98%
Indomethacin ++

COX1, IC50: 0.28 μM

 		+

COX-2, IC50: 14 μM

 		97%
Lornoxicam ++++

COX-1, IC50: 5 nM

 		++++

COX-2, IC50: 8 nM

 		98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

 		+++

COX-2, IC50: 50 nM

 		99%
Asaraldehyde ✔ 98%
Naproxen +

COX-1, IC50: 8.7 μM

 		+

COX-2, IC50: 5.2 μM

 		98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

 		+++

COX-2, IC50: 200 nM

 		98%
NS-398 ++

COX-2, IC50: 3.8 μM

 		95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

 		+++

COX-2, IC50: 150 nM

 		98%+
Nimesulide +

COX-2, IC50: 26 μM

 		98%
Lumiracoxib ++

COX-1, Ki: 3 μM

 		+++

COX-2, Ki: 60 nM

 		98%
Rutaecarpine ✔ 95%
Celecoxib ++++

COX-2, IC50: 40 nM

 		98%
Carprofen ++++

canine COX2, IC50: 30 nM

 		98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

 		++

COX-2 (human), IC50: 3.50 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Celecoxib/塞来昔布 生物活性

靶点

  • COX-2

    COX-2, IC50:40 nM
描述 Cyclooxygenase (COX) is an enzyme that produces precursors to prostaglandins and thromboxanes. It is associated with rheumatoid arthritis (RA), osteoarthritis (OA), and other inflammatory disorders. Celecoxib is a dyaryl heterocyclic inhibitor of COX-2, a subtype of COX that is highly expressed in inflamed tissues. In human dermal fibroblasts, celecoxib inhibited COX-2-mediated production of prostaglandin E2 (PGE2) with an IC50 at 91 nM, compared to its IC50 value of COX-1 inhibition at 2800 nM[6]. When IL-1β-stimulated fibroblast-like synoviocytes were treated by 10 μM celecoxib for 24 hours, the production of PGE2 and the gene expression of COX-2 were significantly decreased compared to non-treated cells[7]. In vivo, celecoxib was orally administrated to male Sprague-Dawley rats 4 hours after carrageenan injection, and it was shown to abrogate carrageenan-induced thermal hyperalgesia with an ED30 value of 0.81 mg/kg. Celecoxib also showed inhibitory effect on lipopolysaccharide-induced pyrexia in rats with an ED30 of 1.3 mg/kg[6]. RA patients who received 40, 200, or 400 mg celecoxib twice daily for 4 weeks presented significantly reduced signs and symptoms[8]. In OA patients, 6-week treatment of 200 mg celecoxib once daily significantly improved their scores on pain satisfaction scales[9].
作用机制 The phenylsulfonamide moiety of celecoxib binds to the side pocket of cyclooxygenase (COX)-2 to prevent the activation of COX-2 to other stimuli[8].

Celecoxib/塞来昔布 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293T cells 4 μM 1 hour To evaluate the effect of Celecoxib on PROKR1 signaling pathway, results showed that Celecoxib selectively activated Gs signaling and increased NR4A2 protein levels by 1.6-fold. J Cachexia Sarcopenia Muscle. 2025 Feb;16(1):e13704.
H1299 cells 40 μM 48 h Evaluate the combined effects of Celecoxib and Aspirin on cell apoptosis, cell cycle distribution, cell proliferation, cell migration, and signaling pathways. Results showed that the combination of Celecoxib and Aspirin significantly inhibited cell proliferation and induced apoptosis compared to either drug alone. Ther Adv Med Oncol. 2020 Sep 17;12:1758835920947976.
A549 cells 40 μM 48 h Evaluate the combined effects of Celecoxib and Aspirin on cell apoptosis, cell cycle distribution, cell proliferation, cell migration, and signaling pathways. Results showed that the combination of Celecoxib and Aspirin significantly inhibited cell proliferation and induced apoptosis compared to either drug alone. Ther Adv Med Oncol. 2020 Sep 17;12:1758835920947976.
SACC-83 cells 98.75 μM( IC50) 12 h To evaluate the inhibitory effects of celecoxib and its derivatives on SACC-83 cells, the results showed that celecoxib could induce apoptosis in tumor cells and effectively suppress tumor cell invasion and migration. Adv Sci (Weinh). 2025 Feb;12(8):e2408751.

Celecoxib/塞来昔布 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Lumbar spine instability model Oral 20 mg/kg Once daily for 1 to 4 weeks Low-dose celecoxib significantly reduced vertebral endplate porosity and induced a latent inhibition of spinal pain at 3 weeks post-treatment, which persisted even after discontinuing treatment. Furthermore, when the prostaglandin E2 concentration was maintained at the physiological level with low-dose celecoxib, endplate porosity was reduced significantly, which was associated with decreased sensory nerve innervation and spinal pain. Bone Res. 2021 Aug 2;9(1):36
Mice High-fat diet-induced obesity model Oral 500, 1000, 1500 ppm From gestation day 5 to weaning To evaluate the effect of Celecoxib on muscle phenotype, results showed that Celecoxib improved muscle phenotype, increased lean mass and grip strength. J Cachexia Sarcopenia Muscle. 2025 Feb;16(1):e13704.
Wistar rats Experimental autoimmune prostatitis (EAP) model Oral gavage 18 mg/kg Once daily for 8 weeks To evaluate the anti-inflammatory efficacy of celecoxib in EAP model rats, results showed that celecoxib effectively alleviated depression-like behavior and sexual dysfunction in EAP model rats, and reduced serum levels of inflammatory factors IL-1β and TNF-α. Front Immunol. 2020 Sep 9;11:574212
Wistar rats 1,2-dimethylhydrazine-induced colorectal cancer model Oral 5 mg/kg Once daily for 12 weeks To evaluate the antitumor activity of CLX-ES-PEI-UENVs in the DMH-induced colorectal cancer model, showing significant efficacy through up-regulation of the Wnt/β-catenin pathway. Int J Pharm X. 2023 Dec 20;7:100225
Nude mice Human NSCLC xenograft model Intraperitoneal injection 50 mg/kg Every other day for 28 days Evaluate the inhibitory effect of Celecoxib and Aspirin on tumor growth. Results showed that the combination of Celecoxib and Aspirin significantly inhibited tumor growth and prolonged tumor doubling time compared to either drug alone. Ther Adv Med Oncol. 2020 Sep 17;12:1758835920947976.
NOD-SCID mice Pulmonary metastasis model Intraperitoneal injection 5 mg/kg Once every 2 days for 8 weeks To evaluate the inhibitory effects of celecoxib and its derivatives on SACC lung metastasis, the results showed that celecoxib significantly reduced the number of lung metastasis nodules. Adv Sci (Weinh). 2025 Feb;12(8):e2408751.
C57BL/6J mice GL261 glioma model Oral 25 mg/kg Daily for 66 days Celecoxib, as a COX-2 inhibitor, selectively inhibits the production of prostaglandins, reversing immunosuppression in the tumor microenvironment and enhancing immunotherapy efficacy. The experimental results showed that celecoxib played a critical role in the vMyx-IL15R α-tdTr combination therapy, significantly increasing CD8+ T cell infiltration and reducing Treg cell infiltration, thereby improving treatment outcomes. Clin Cancer Res. 2020 May 1;26(9):2216-2230
Mice Non-invasive ACL rupture model Intraperitoneal injection 10 mg/kg Daily for 7 days To investigate the effects of early mechanical unloading and celecoxib treatment on post-traumatic osteoarthritis progression. Results showed that celecoxib treatment reduced osteophyte formation at 28 days but did not significantly affect early protease activity or synovitis. Osteoarthritis Cartilage. 2021 Dec;29(12):1709-1719

Celecoxib/塞来昔布 动物研究

Dose Rat: 10 mg/kg - 50 mg/kg[3] (p.o.) Dog: 7.5 mg/kg - 25 mg/kg[4] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[5]
Dose 10 mg/kg
Administration p.o./i.v.
F 64.5% (p.o.)
Vd 1860 ml/kg (i.v.)
T1/2 3.67 h (p.o.)
3.49 h (i.v.)
Tmax 3 h (p.o.)
Cmax 2.01 μg/ml (p.o.)
4.87 μg/ml (i.v..)
AUC0→∞ 18.5 μg·h/ml (p.o.)
28.7 μg·h/ml (i.v.)

Celecoxib/塞来昔布 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00653250 Lung Cancer Not Applicable Completed - -
NCT00533247 Postoperative Pain Not Applicable Unknown - Canada, British Columbia ... 展开 >> Not yet recruiting Vancouver, British Columbia, Canada Contact: Adam Zanbilowicz, BA DPM MS    604-885-8803    zanbilowicz@pol.net 收起 <<
NCT00153660 Arthritis Car... 展开 >>diovascular Diseases Cerebrovascular Disorders 收起 << Phase 3 Completed - China, Hong Kong ... 展开 >> Endoscopy Center, Prince of Wales Hospital Shatin, Hong Kong, China 收起 <<

Celecoxib/塞来昔布 参考文献

[1]Safaeian L, Hajhashemi V, et al. The effect of celecoxib on blood pressure and plasma oxidant/antioxidant status in co-administration with glucocorticoid in rat. Biomed Pharmacother. 2018 Dec;108:1804-1808.

[2]Paulson SK, Vaughn MB, et al. Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption. J Pharmacol Exp Ther. 2001 May;297(2):638-45.

[3]CELEBREX

[4]55(7):394-402.

[5]42(6):499-506.

[6]Yoshino T, Kimoto A, Kobayashi S, Noguchi M, Fukunaga M, Hayashi A, Miyata K, Sasamata M. Pharmacological profile of celecoxib, a specific cyclooxygenase-2 inhibitor. Arzneimittelforschung. 2005;55(7):394-402.

[7]Kawashima M, Ogura N, Akutsu M, Ito K, Kondoh T. The anti-inflammatory effect of cyclooxygenase inhibitors in fibroblast-like synoviocytes from the human temporomandibular joint results from the suppression of PGE2 production. J Oral Pathol Med. 2013 Jul;42(6):499-506.

Celecoxib/塞来昔布 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.11mL

2.62mL

1.31mL

26.22mL

5.24mL

2.62mL

Celecoxib/塞来昔布 技术信息

CAS号169590-42-5
分子式C17H14F3N3O2S
分子量 381.37
SMILES Code O=S(C1=CC=C(N2N=C(C(F)(F)F)C=C2C3=CC=C(C)C=C3)C=C1)(N)=O
MDL No. MFCD00941298
别名 塞来西布 ;SC 58635; YM-177; Celebrex
运输蓝冰
InChI Key RZEKVGVHFLEQIL-UHFFFAOYSA-N
Pubchem ID 2662
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

DMSO: 50 mg/mL(131.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 二
方案 三
方案 四

Tags: Celecoxib | 169590-42-5 | SC 58635 | SC58635 | SC-58635 | COX-2inhibitor | Immunology/Inflammation | COX | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Celecoxib/塞来昔布 纯度/质量文件 | Celecoxib/塞来昔布 亚型比较 | Celecoxib/塞来昔布 生物活性 | Celecoxib/塞来昔布 动物研究 | Celecoxib/塞来昔布 临床数据 | Celecoxib/塞来昔布 参考文献 | Celecoxib/塞来昔布 实验方案 | Celecoxib/塞来昔布 技术信息

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