Diclofenac potassium (Voltarol; Voltaren), the potassium salt of diclofenac, is a nonsteroidal anti-inflammatory drug (NSAID) that is able to reduce inflammation and to be used as an analgesic reducing pain in certain conditions. It acts 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.
Physicochemical Properties
| Molecular Formula | C14H10CL2KNO2 |
| Molecular Weight | 334.2390 |
| Exact Mass | 332.972 |
| CAS # | 15307-81-0 |
| Related CAS # | Diclofenac;15307-86-5;Diclofenac diethylamine;78213-16-8;Diclofenac Sodium;15307-79-6 |
| PubChem CID | 23667642 |
| Appearance | White to off-white solid powder |
| Boiling Point | 412ºC at 760 mmHg |
| Melting Point | 156-158ºC |
| Flash Point | 203ºC |
| Vapour Pressure | 1.59E-07mmHg at 25°C |
| LogP | 3.102 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 3 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 20 |
| Complexity | 310 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | KXZOIWWTXOCYKR-UHFFFAOYSA-M |
| InChi Code | InChI=1S/C14H11Cl2NO2.K/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 |
| Chemical Name | potassium;2-[2-(2,6-dichloroanilino)phenyl]acetate |
| HS Tariff Code | 2934.99.9001 |
| Storage |
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. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | 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]. |
| ln Vivo | 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 Assay |
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. 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: po (po (oral gavage)) bid, for 5 days Experimental Results: It resulted in a significant increase in 51Cr excretion in feces. 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]. 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. |
| Additional Infomation |
Diclofenac potassium is the potassium salt of diclofenac. It contains a diclofenac(1-). Diclofenac Potassium is the potassium salt form of diclofenac, a benzene acetic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and anti-inflammatory activity. Diclofenac potassium 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 (has active moiety). |
Solubility Data
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~299.19 mM) H2O : ~14.29 mg/mL (~42.75 mM) H2O : ~14.29 mg/mL (~42.75 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.48 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.48 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (7.48 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9919 mL | 14.9593 mL | 29.9186 mL | |
| 5 mM | 0.5984 mL | 2.9919 mL | 5.9837 mL | |
| 10 mM | 0.2992 mL | 1.4959 mL | 2.9919 mL |