双氯芬酸的 IC50 为 7±3 nM，可有效抑制 U937 细胞中 COX-1 介导的微粒体前列腺素合成[1]。当暴露于双氯芬酸钠（1–60 μM；1 天）时，神经干细胞 (NSC) 会发生浓度依赖性细胞凋亡 [3]。当暴露于双氯芬酸钠 (10–60 μM) 六小时时，克隆（激活）的 caspase-3 表达更多 [3]。

双氯芬酸钠（3 mg/kg，bid）连续五天可大大增加大鼠粪便 51Cr 的排泄。在松鼠猴中也观察到了这种效果，松鼠猴每天两次服用 1 mg/kg，持续四天 [1]。在 Wistar 大鼠中，在炎症发生前口服双氯芬酸钠 (10 mg/kg) 可发挥抗炎作用 [1]。

细胞活力测定[3]
细胞类型：神经干细胞 (NSC)
测试浓度：1、3、10、30、60 μM
孵育时间： 1 天
实验结果：细胞死亡的诱导具有浓度依赖性，并且在浓度高达 60 μM 时效果不饱和。

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蛋白质印迹分析[3]
细胞类型： 神经干细胞 (NSC)
测试浓度： 10、30 或 60 μM
孵育持续时间：6小时
实验结果：caspase-3的激活以浓度依赖性方式增加。

Animal/Disease Models: Male SD (Sprague-Dawley) rats (150±200 g)[1]
Doses: 3 mg/kg
Route of Administration: Oral administration, bid, for 5 days
Experimental Results: Resulted in a significant increase in faecal 51Cr excretion.

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Animal/Disease Models: Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2]
Doses: 10 mg/kg
Route of Administration: Administered via oral route just prior to induction of inflammation
Experimental Results: demonstrated in vivo anti-inflammatory activity (% edema inhibition= 29.2, 1 h; 22.2, 3 h; 20, 6 h).

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Data on excretion of diclofenac into milk are poor, but the drug has a short half-life and little glucuronide metabolite formation. Levels in milk appear to be quite low. Most reviewers consider diclofenac to be acceptable during breastfeeding. Other agents having more published information may be preferred, especially while nursing a newborn or preterm infant.
Maternal use of diclofenac topical gel or eye drops would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
◉ Effects in Breastfed Infants
In one study, 30 mothers undergoing elective cesarean section were allowed to use 25 mg diclofenac suppositories along with either spinal or spinal and epidural anesthesia with a local anesthetic after delivery. The spinal anesthetic group used an average of 56 mg of diclofenac on the day of delivery and 33 mg on the next day whereas the women receiving both spinal and epidural anesthesia used 21 and 18 mg. No mention was made of adverse effects on the breastfed infants.
A breastfed infant developed urticaria on day 15 of life. Her mother had been taking diclofenac (dosage unspecified) for pain since her cesarean section delivery. Diclofenac is a possible cause of the urticaria; however, the infant had also received hepatitis B vaccination 7 days before and the authors thought that it was a more likely cause of the reaction.
◉ Effects on Lactation and Breastmilk
A randomized, double-blind study was performed in pregnant women scheduled for cesarean section under spinal anesthesia with bupivacaine and fentanyl. Patients received either 100 mg diclofenac (n = 100), 100 mg tramadol (n = 100) or placebo (glycerin suppositories) n = 100, all given as rectal suppositories every 8 hours for the first 24 hours after surgery. The time to initiate breastfeeding was significantly shorter among mothers who received diclofenac than a placebo, 1.5 vs 4.1 hours with breastfeeding support and 3.5 vs 6.2 hours without support. Diclofenac was slightly more effective than tramadol among mothers who received no support (3.5 vs 3.7 hours).

[1]. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.

[2]. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80.

[3]. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95.

Diclofenac sodium is the sodium salt of diclofenac. It contains a diclofenac(1-).
Diclofenac Sodium is the sodium salt form of diclofenac, a benzene acetic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and anti-inflammatory activity. Diclofenac sodium is a non-selective reversible and competitive inhibitor of cyclooxygenase (COX), subsequently blocking the conversion of arachidonic acid into prostaglandin precursors. This leads to an inhibition of the formation of prostaglandins that are involved in pain, inflammation and fever.
A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.
See also: Diclofenac (brandname of); Omeprazole (has active ingredient); Capsicum Oleoresin (has active ingredient) ... View More ...

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Drug Indication
Treatment of inflammation, Treatment of pain

C14H10CL2NNAO2

318.13

316.998

15307-79-6

Diclofenac;15307-86-5;Diclofenac diethylamine;78213-16-8;Diclofenac-d4 sodium;154523-54-3;Diclofenac potassium;15307-81-0;Diclofenac-13C6 sodium heminonahydrate;Diclofenac-13C6 Sodium;1261393-73-0

5018304

White to off-white solid powder

412ºC at 760 mmHg

288-290°C

203ºC

3.102

52.16

1

3

4

20

310

0

KPHWPUGNDIVLNH-UHFFFAOYSA-M

1S/C14H11Cl2NO2.Na/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19;/h1-7,17H,8H2,(H,18,19);/q;+1/p-1

Benzeneacetic acid, 2-((2,6-dichlorophenyl)amino)-, monosodium salt

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: 4.55 mg/mL (14.30 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。 (<60°C).

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。