塞来西布

塞来西布，Celecoxib，CAS No. :169590-42-5，纯度: 99.98%，是一种非甾体抗炎剂，是一种 COX-2 抑制剂 (IC50=40 nM)，具有选择性。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。

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塞来西布

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抑制剂

目录号

T0466

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塞来西布，Celecoxib (SC 58635) 是一种非甾体抗炎剂，是一种 COX-2 抑制剂 (IC₅₀=40 nM)，具有选择性。Celecoxib 具有抗炎和止痛活性，可以用于治疗骨关节炎、类风湿性关节炎、急性疼痛等。

生物活性

产品描述	Celecoxib (SC 58635) is a non-steroidal anti-inflammatory agent, a COX-2 inhibitor (IC₅₀=40 nM), with selectivity. Celecoxib has anti-inflammatory and analgesic activity and can be used for the treatment of osteoarthritis, rheumatoid arthritis, and acute pain.
靶点活性 (IC₅₀)	COX-2:40 nM, Hone-1 cells:49.68 ± 1.12 μM, COX-1:15 μM, HK-1 cells:51.74 ± 3.89 μM, CNE-2 cells:41.04 ± 1.22 μM, A2058 cells:63 ± 4 µM
体外活性	方法：鼻咽癌 (NPC) 细胞系 HNE1 和 CNE1-LMP1 用 Celecoxib (5-75 µM) 处理 48 h，使用 MTT assay 检测细胞活力。结果：Celecoxib 的抑制作用以剂量依赖的方式发生。Celecoxib 在 HNE1 和 CNE1-LMP1 中的平均 IC₅₀ 值分别为 32.86±1.13 µmol/L 和 61.31±4.30 µmol/L。^[1] 方法：人正常肝细胞 L02 用 PA (200 µM) 和 Celecoxib (5-40 µM) 处理 24 h，使用 Western Blot 检测靶点蛋白表达水平。结果：PA 诱导 COX-2 上调，LC3 II/I 和 p62 的蛋白质表达增加。PA和 Celecoxib 联用，COX-2 和 p62 的蛋白水平显著降低，LC3 II/I 增加。^[2]
体内活性	方法：为测试是否能降低放射性肺炎的死亡率，将 Celecoxib (25 mg/kg in 0.5% methyl cellulose and 0.025% Tween 20 in sterile water) 灌胃给药给局部胸部照射 (LTI) 的 C3Hf/KamLaw 小鼠。从 LTI 当天或 40 或 80 天后开始给药，每天两次，持续四十天。结果：Celecoxib 相对于 LTI 的时间决定了疗效。只有当 Celecoxib 在 LTI 后 80 天开始使用时，死亡时间才能显著缩短，这与肺炎的表达时间相对应。对于这些小鼠，死亡率的降低被量化为治疗组与未治疗组的死亡率的风险比为 0.36。^[3]
激酶实验	COX enzyme assay in vitro: Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.
细胞实验	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 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. 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 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. 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.(Only for Reference)
别名	塞来昔布, 塞来西布, SC 58635

化学信息

分子量	381.372
分子式	C₁₇H₁₄F₃N₃O₂S
CAS No.	169590-42-5
Smiles	CC1=CC=C(C=C1)C1=CC(=NN1C1=CC=C(C=C1)S(N)(=O)=O)C(F)(F)F
密度	1.43 g/cm3 (Predicted)

产品组分

内容	型号	规格	储存温度
塞来西布	T0466-01	25mg	-20°C
塞来西布	T0466-02	50mg	-20°C
塞来西布	T0466-03	100mg	-20°C
塞来西布	T0466-04	200mg	-20°C
塞来西布	T0466-05	1g	-20°C
依达奴林	T0466-06	1mLx10mM in DMSO	-20°C
操作手册	1	1	常温

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FAQ
1.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.

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

3.Hunter NR, et al. Mitigation and treatment of radiation-induced thoracic injury with a cyclooxygenase-2 inhibitor, celecoxib. Int J Radiat Oncol Biol Phys. 2013 Feb 1;85(2):472-6.

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