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> Diclofenac (Sodium) [15307-79-6]

Diclofenac (Sodium) [15307-79-6]

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Referencia HY-15037-5g

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Descripciòn

Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells[1], and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively[2]. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade[3].

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 μM (IC50)

Ovine COX-1

5.1 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
Erythrocyte EC50
11.7 μg/mL
Compound: Diclofenac sodium
Anti-inflammatory activity in human red blood cells assessed as stabilization of cell membrane
Anti-inflammatory activity in human red blood cells assessed as stabilization of cell membrane
[PMID: 32485533]
HT-29 IC50
137.1 μM
Compound: Diclofenac sodium
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
[PMID: 32485532]
RAW264.7 IC50
10.27 μM
Compound: Diclofenac sodium
Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
[PMID: 33892270]
RAW264.7 IC50
12.19 μM
Compound: Diclofenac sodium
Inhibition of LPS-induced 15(S)-HETE production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
Inhibition of LPS-induced 15(S)-HETE production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
[PMID: 33892270]
RAW264.7 IC50
12.91 μM
Compound: Diclofenac sodium
Inhibition of LPS-induced IL-6 production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
Inhibition of LPS-induced IL-6 production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA
[PMID: 33892270]
RAW264.7 IC50
25.51 μM
Compound: Diclofenac sodium
Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced intracellular ROS production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by DCFH-DA staining based fluorescence analysis
Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced intracellular ROS production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by DCFH-DA staining based fluorescence analysis
[PMID: 33892270]
RAW264.7 IC50
331 μM
Compound: Diclofenac sodium
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess reagent based analysis
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess reagent based analysis
[PMID: 38805684]
RAW264.7 IC50
36.28 μM
Compound: Diclofenac sodium
Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by DAF-FM based fluorescence analysis
Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by DAF-FM based fluorescence analysis
[PMID: 33892270]
THP-1 IC50
200.9 μM
Compound: Diclofenac sodium
Cytotoxicity against PMA/LPS-challenged human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
Cytotoxicity against PMA/LPS-challenged human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
[PMID: 32485532]
In Vitro

Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7±3 nM[1].
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner[3].
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Diclofenac Sodium Related Antibodies

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

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days[1].
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Peso molecular

318.13

Fòrmula

C14H10Cl2NNaO2
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[Na])CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

DMSO : 125 mg/mL (392.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 10 mg/mL (31.43 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 4.55 mg/mL (14.30 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
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