Diclofenac是一种强效的非选择性环氧化酶（COX）抑制剂，在CHO细胞中对人源COX-1和COX-2的IC₅₀值分别为4nM和1.3nM；对羊源COX-1和COX-2的IC₅₀值分别为5.1μM和0.84μM。
Cas No.:15307-86-5
Sample solution is provided at 25 µL, 10mM.
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Diclofenac is a potent, non-selective cyclooxygenase (COX) inhibitor, with IC₅₀ values of 4nM and 1.3nM for human COX-1 and COX-2, respectively, in CHO cells, and 5.1μM and 0.84μM for ovine COX-1 and COX-2, respectively[1][2]. Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) widely used in clinical practice for its anti-inflammatory, analgesic, and antipyretic effects[3].
In vitro, Diclofenac (10-200mM; 24-72h) inhibited the proliferation of HepG2 and Hep3B cells in a dose-dependent manner. After 48h of treatment at 50mM, the inhibition rates are 40.47% and 54.49% for HepG2 and Hep3B cells, respectively, with IC₅₀ values of 70.54mM and 48.39mM[4]. Diclofenac (10-200mM; 24-72h) also upregulated COX-2 mRNA expression in both cell lines[4]. Diclofenac (0-60μM, 24-48h) dose-dependently inhibited neurite outgrowth and neuronal differentiation of neural stem cells (NSCs), and induced NSC death via activation of the caspase signaling cascade[3].
In vivo, Administration of Diclofenac (3mg/kg; twice daily for 5 days; p.o.) in male SD rats disrupted gastrointestinal integrity, resulting in a significant increase in fecal ⁵¹Cr excretion[1]. Oral Diclofenac (3mg/kg/d) for 15 days significantly reduced edema by day 3 and exhibited anti-hyperalgesic effects by day 9 in the rat model of repeated arthritis[5].
References:
[1] Riendeau D, Percival MD, Boyce S, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997;121(1):105-117.
[2] Labib MB, Sharkawi SMZ, El-Daly M. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018;80:70-80.
[3] Kudo C, Kori M, Matsuzaki K, et al. Diclofenac inhibits proliferation and differentiation of neural stem cells. Biochem Pharmacol. 2003;66(2):289-295.
[4] Chen NN, Wu SG. Nan Fang Yi Ke Da Xue Xue Bao. 2006;26(6):814-817.
[5] Peter-Szabo, Mihaly et al. “Quantitative characterization of a repeated acute joint inflammation model in rats.” Clinical and experimental pharmacology & physiology vol. 34,5-6 (2007): 520-6.
Diclofenac是一种强效的非选择性环氧化酶（COX）抑制剂，在CHO细胞中对人源COX-1和COX-2的IC₅₀值分别为4nM和1.3nM；对羊源COX-1和COX-2的IC₅₀值分别为5.1μM和0.84μM[1][2]。Diclofenac是一种非甾体抗炎药（NSAID），因其具有抗炎、镇痛和解热作用而被广泛应用于临床[3]。
体外实验中，Diclofenac（10-200mM；24-72h）以剂量依赖性方式抑制HepG2和Hep3B细胞的增殖。在50mM处理48h后，对HepG2和Hep3B细胞的抑制率分别为40.47%和54.49%，其IC₅₀值分别为70.54mM和48.39mM[4]。Diclofenac（10-200mM；24-72h）还上调了这两种细胞系中的COX-2 mRNA表达水平[4]。Diclofenac（0-60μM；24-48h）以剂量依赖的方式抑制神经干细胞（NSCs）的神经突起生长及向神经元的分化，并通过激活caspase信号级联反应诱导NSCs死亡[3]。
体内实验中，Diclofenac（3mg/kg；每日两次连续5天；口服）在雄性SD大鼠中可破坏胃肠道完整性，导致粪便中⁵¹Cr排泄显著增加[1]。口服Diclofenac（3mg/kg/天）连续15天在反复关节炎大鼠模型中于第3天显著减轻水肿，在第9天表现出抗痛觉作用[5]。
| Cell experiment [1]: | |
Cell lines | HepG2, Hep3B and QSG-7701 |
Preparation Method | After exposure to Diclofenac at various concentrations (10-200mM) for 24, 48 and 72h, the cell proliferation was analyzed by Cell Counting Kit-8 (CCK-8) assay and mRNA expression determined by semi-quantitative reverse transcription-polymerase chain reaction (RT-PCR). |
Reaction Conditions | 10-200mM; 24, 48 and 72h |
Applications | Diclofenac exposure for 24, 48 and 72h significantly inhibited HepG2 and Hep3B cell proliferation in a concentration-dependent manner, with inhibition rate of 40.47% and 54.49% after 48h exposure to 50mM and IC50 of 70.54 and 48.39mM, respectively. A much weaker anti-proliferative effect on QSG-7701 cells was shown, with IC50 of 189.91mM after 48h exposure to Diclofenac. RT-PCR detected COX-2 mRNA in HepG2 and Hep3B cells, but hardly in QSG-7701 cells. Treatment with Diclofenac resulted in elevated COX-2 mRNA expression both in HepG2 and Hep3B cells. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats were dosed orally with Diclofenac 3mg/kg twice daily (b.i.d.) for 5 days. A plasma sample was obtained 1h after the morning dose on day 4 for measurement of drug concentration. Immediately after the administration of the last dose on day 5, the rats were injected via a tail vein with 0.5ml of 51Cr-labelled red blood cells from a donor rat after incubation with sodium 51chromate. The rats were placed individually in metabolism cages with food and water ad libitum. Faeces were collected for a 48h period and 51Cr faecal excretion was calculated as a % of total injected dose (20μCi per animal) |
Dosage form | 3mg/kg; b.i.d.; p.o. |
Applications | Administration of Diclofenac at 3mg/kg, b.i.d., for 5 days resulted in a significant increase in faecal 51Cr excretion. |
References: | |
| Cas No. | 15307-86-5 | SDF | |
| 别名 | 双氯芬酸 | ||
| 化学名 | 2-(2-((2,6-dichlorophenyl)amino)phenyl)acetic acid | ||
| Canonical SMILES | ClC1=C(NC2=CC=CC=C2CC(O)=O)C(Cl)=CC=C1 | ||
| 分子式 | C14H11Cl2NO2 | 分子量 | 296.15 |
| 溶解度 | ≥ 14.8mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3767 mL | 16.8833 mL | 33.7667 mL |
| 5 mM | 675.3 μL | 3.3767 mL | 6.7533 mL |
| 10 mM | 337.7 μL | 1.6883 mL | 3.3767 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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