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Purity: ≥98%
Diclofenac (formerly GP-45840; Voltarol; Voltaren) is a potent nonsteroidal anti-inflammatory drug (NSAID), acting as a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used to relieve pain and reduce swelling in flammation. Diclofenac inhibits Wnt/beta-catenin signaling without altering the level of beta-catenin protein and reduces the expression of beta-catenin/TCF-dependent genes. Diclofenac induces the degradation of IkappaBalpha, which increases free nuclear factor kappaB (NF-kappaB) in colon cancer cells.
| ln Vitro |
At an IC50 of 7±3 nM, diclofenac efficiently explodes COX-1-mediated microsomal formation in U937 cells[1]. Neural stem cells (NSCs) are killed by diclofenac (1–60 μM; 1 day) in a concentration-dependent way. Every six days, caspase-3 expression is increased by diclofenac (10–60 μM; 1).
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| ln Vivo |
Squirrel monkeys administered 1 mg/kg twice daily for 4 days likewise showed a substantial increase in fecal Cr excretion following treatment with diclofenac (3 mg/kg, bid) for 5 days [1]. Wistar rats treated with diclofenac (10 mg/kg; administered prior to triggering factors passing via the route medication) show anti-inflammatory action [1].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Neural Stem cells (NSCs) Tested Concentrations: 1, 3, 10, 30, 60 μM Incubation Duration: 1 day Experimental Results: Induction of cell death is concentration-dependent and occurs at concentrations up to 60 μM The effect is not saturated. 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 Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (150±200 g) [1]
Doses: 3 mg/kg Route of Administration: Oral administration, bid, for 5 days Experimental Results: Caused a significant increase in fecal 51Cr excretion. 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))). |
| References |
[1]. Riendeau D, et al. 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]. Labib MB, et al. 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]. Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95. |
| Molecular Formula |
C14H11CL2NO2
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|---|---|
| Molecular Weight |
296.15
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| Exact Mass |
295.01668
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| CAS # |
15307-86-5
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| Related CAS # |
Diclofenac diethylamine;78213-16-8;Diclofenac-d4;153466-65-0;Diclofenac Sodium;15307-79-6;Diclofenac potassium;15307-81-0;Diclofenac-13C6;1261393-71-8
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| SMILES |
C1=CC=C(C(=C1)CC(=O)O)NC2=C(C=CC=C2Cl)Cl
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| InChi Key |
DCOPUUMXTXDBNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11Cl2NO2/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)
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| Chemical Name |
2-[2-(2,6-dichloroanilino)phenyl]acetic acid
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| Synonyms |
Diclofenac acid Dichlofenac Voltarol Voltaren
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~422.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.02 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.02 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3767 mL | 16.8833 mL | 33.7667 mL | |
| 5 mM | 0.6753 mL | 3.3767 mL | 6.7533 mL | |
| 10 mM | 0.3377 mL | 1.6883 mL | 3.3767 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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