| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C14H10Cl2KNO2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Diclofenac potassium is a potent, nonselective anti-inflammatory agent that acts as a COX inhibitor, with IC50 values of 4 nM and 1.3 nM against human COX-1 and COX-2 in CHO cells[1], and 5.1 μM and 0.84 μM against ovine COX-1 and COX-2, respectively[2]. It also induces apoptosis of neural stem cells (NSCs) through activation of the caspase cascade[3]. It is supplied as a white to off-white solid (C14H10Cl2KNO2, MW 334.24) at 99.85% purity.
Physical & Chemical Properties
| CAS Number | 15307-81-0 |
|---|---|
| Molecular Formula | C14H10Cl2KNO2 |
| Molecular Weight | 334.24 g/mol |
| Purity | 99.85% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(O[K])CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl |
| Target | Human COX-2, Human COX-1, Ovine COX-2, Ovine COX-1 |
| Signaling Pathway | Immunology/Inflammation; Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (299.19 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 14.29 mg/mL (42.75 mM; Requires sonication and warming and heat to 60°C) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
[1][2]
|
Human COX-2 1.3 nM (IC50, in CHO cells) |
Human COX-1 4 nM (IC50, in CHO cells) |
Ovine COX-2 0.84 nM (IC50) |
Ovine COX-1 5.1 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (299.19 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 14.29 mg/mL (42.75 mM) | requires sonication and warming and heat to 60°C |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (7.48 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (7.48 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (7.48 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Diclofenac effectively blocks COX-1-mediated prostanoid production in U937 cell microsomes (IC50 of 7±3 nM)[1]. At 1-60 μM for 1 day, Diclofenac causes neural stem cell (NSC) death in a concentration-dependent manner[3]. At 10-60 μM for 6 hours, it raises the expression of cleaved (activated) caspase-3[3].
Cell Viability Assay[3]
| Cell Line | Neural stem cells (NSCs) |
|---|---|
| Concentration | 1, 3, 10, 30, 60 μM |
| Incubation Time | 1 day |
| Result | 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 Line | Neural stem cells (NSCs) |
|---|---|
| Concentration | 10, 30 or 60 μM |
| Incubation Time | 6 hours |
| Result | The activation of caspase-3 was increased in a concentration-dependent manner. |
In Vivo
Faecal 51Cr excretion rises significantly in rats given Diclofenac at 3 mg/kg, b.i.d., for 5 days; the same effect is seen in squirrel monkeys given 1 mg/kg twice daily for 4 days[1]. In Wistar rats, Diclofenac (10 mg/kg; given orally just before induction of inflammation) shows in vivo anti-inflammatory activity[1].
| Animal Model | Male Sprague-Dawley rats (150±200 g)[1] |
|---|---|
| Dosage | 3 mg/kg |
| Administration | Oral administration, b.i.d., for 5 days |
| Result | Resulted in a significant increase in faecal 51Cr excretion. |
| Animal Model | Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | Administered via oral route just prior to induction of inflammation |
| Result | Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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J Phys Chem Solids. 2017 October;109:117-123.