Diclofenac, with an IC50 of 7±3 nM, can efficiently inhibit COX-1-mediated prostaglandin synthesis in U937 cell microsomes[1]. Neural stem cell (NSC) mortality is concentration-dependently induced by diclofenac (1-60 μM; 1 day) [3]. The expression of cleaved (activated) caspase-3 is increased by 10–60 μM diclofenac when given for six hours [3].

Rats treated with diclofenac (3 mg/kg twice daily for 5 days) had a considerable increase in 51Cr excreted in their feces; squirrel monkeys treated with 1 mg/kg twice daily for 4 days also experienced this effect [1]. In vivo anti-inflammatory efficacy has been seen in Wistar rats treated with 10 mg/kg of diclofenac orally prior to induction of inflammation [1].

Cell viability assay [3]
Cell Types: Neural stem cells (NSC)
Tested Concentrations: 1, 3, 10, 30, 60 μM
Incubation Duration: 1 day
Experimental Results: The induction of cell death is concentration-dependent, and the effect is not saturated at a certain concentration . Concentrations up to 60 μM.

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Western Blot Analysis[3]
Cell Types: Neural Stem Cells (NSC)
Tested Concentrations: 10, 30 or 60 μM
Incubation Duration: 6 hrs (hours)
Experimental Results: Activation of caspase-3 increased in a concentration-dependent manner.

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

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Animal/Disease Models: Wistar rat (150-175 g) formalin-induced rat paw edema model [2]
Doses: 10 mg/kg
Route of Administration: By oral route before inducing inflammation
Experimental Results: Shown in vivo Anti-inflammatory activity (% edema inhibition = 29.2 at 1 hour; 22.2 at 3 hrs (hrs (hours)); 20 at 6 hrs (hrs (hours))).

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.

C18H22CL2N2O2

369.2855

368.105

78213-16-8

Diclofenac;15307-86-5;Diclofenac-d4;153466-65-0;Diclofenac Sodium;15307-79-6;Diclofenac potassium;15307-81-0

115087

White to off-white solid powder

412ºC at 760 mmHg

145-148ºC

203ºC

5.443

3

4

6

24

315

0

ZQVZPANTCLRASL-UHFFFAOYSA-N

InChI=1S/C14H11Cl2NO2.C4H11N/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19;1-3-5-4-2/h1-7,17H,8H2,(H,18,19);5H,3-4H2,1-2H3

2-[2-(2,6-dichloroanilino)phenyl]acetic acid;N-ethylethanamine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

DMSO : ~150 mg/mL (~406.18 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)