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Purity: ≥98%
Diclofenac Sodium (Abitren, Blesin, Delimon, Allvoran, Berifen, Delphimix, Voltaren, Voltarol; Assaren, Batafil, GP-45840) is a nonsteroidal anti-inflammatory drug (NSAID), acting as a non-selective COX inhibitor with potential anti-inflammatory activity. It inhibits COX-1/2 with IC50 of 0.5 μg/ml and 0.5 μg/ml in intact cells, respectively, and is 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 |
Diclofenac, with an IC50 of 7±3 nM, efficiently inhibits COX-1-mediated microsomal synthesis of prostaglandins in U937 cells[1]. Neural stem cells (NSCs) undergo concentration-dependent apoptosis when exposed to diclofenac sodium (1–60 μM; 1 day) [3]. Cloned (activated) caspase-3 is expressed more when exposed to Diclofenac Sodium (10–60 μM) for six hours [3].
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ln Vivo |
Rats' fecal 51Cr excretion is greatly increased by diclofenac sodium (3 mg/kg, bid) for five days. This effect was also seen in squirrel monkeys, who received 1 mg/kg twice daily for four days [1]. In Wistar rats, oral administration of Diclofenac Sodium (10 mg/kg) prior to development of inflammation exhibits 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 was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM. Western Blot Analysis[3] Cell Types: Neural stem cells (NSCs) Tested Concentrations: 10, 30 or 60 μM Incubation Duration: 6 hrs (hours) Experimental Results: The activation of caspase-3 was increased in a concentration-dependent manner. |
Animal Protocol |
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. 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). |
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 |
C14H10CL2NNAO2
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Molecular Weight |
318.13
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CAS # |
15307-79-6
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Related CAS # |
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
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SMILES |
ClC1C([H])=C([H])C([H])=C(C=1N([H])C1=C([H])C([H])=C([H])C([H])=C1C([H])([H])C(=O)[O-])Cl.[Na+]
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InChi Key |
KPHWPUGNDIVLNH-UHFFFAOYSA-M
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InChi Code |
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
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Chemical Name |
Benzeneacetic acid, 2-((2,6-dichlorophenyl)amino)-, monosodium salt
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 4.55 mg/mL (14.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1434 mL | 15.7168 mL | 31.4337 mL | |
5 mM | 0.6287 mL | 3.1434 mL | 6.2867 mL | |
10 mM | 0.3143 mL | 1.5717 mL | 3.1434 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.