Diclofenac

Name: Diclofenac
Brand: MedChemExpress
SKU: HY-15036
Rating: 5.0 (24 reviews)

Cat. No.: HY-15036 Purity: 99.92%: Data Sheet
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Diclofenac 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, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

For research use only. We do not sell to patients.

CAS No. : 15307-86-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	In-stock	Estimated Time of Arrival: December 31
50 g	Get quote

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Based on 24 publication(s) in Google Scholar

Other Forms of Diclofenac:

24 Publications Citing Use of MCE Diclofenac

Cell Proliferation/Viability Assay

Flow Cytometry

Cell Imaging/Staining

: Diclofenac purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066.; KATOIII and KATO/DDP were treated with different concentration of Diclofenac (DCF) (0–1000 µM) for 48 h, and cell viability was assessed.

: Diclofenac purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066.; The KATO/DDP cells were treated with Cisplatin alone or cisplatin in combination with Diclofenac (DCF) at 10 or 20 µM for 24 h, at 37 °C. The apoptosis cells were detected by using annexin V and PI staining and analyzed by flow cytometer.

: Diclofenac purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066.; The combination effect of Diclofenac (DCF) (0, 5, 10, 20 μM) and Cisplatin on the expression of cleaved PARP in KATO/DDP cells was examined by Western blot analysis.

: Diclofenac purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 11;23(20):12066.; The formation of autophagic vacuoles in KATO/DDP cells increased from 27% to 39% and 45% in cotreatments involving cisplatin and Diclofenac (DCF) at 10 and 20 μM, respectively, when compared with treatment of cisplatin alone.

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Biological Activity
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Description

Diclofenac 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 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
CHO	IC₅₀	4 μM Compound: Diclofenac	TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	[PMID: 10991954]
Erythrocyte	IC₅₀	0.942 μM Compound: Diclofenac	Anti-inflammatory activity in human RBC assessed as membrane stabilization Anti-inflammatory activity in human RBC assessed as membrane stabilization	[PMID: 28818769]
HEK293	EC₅₀	56 μM Compound: DCF	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay	[PMID: 30878828]
HEK293	IC₅₀	> 500 μM Compound: diclofenac	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HUVEC	IC₅₀	0.75 mM Compound: Diclofenac	Antiinflammatory activity in HUVEC assessed as inhibition of LPS-induced ICAM1 expression by cell-ELISA Antiinflammatory activity in HUVEC assessed as inhibition of LPS-induced ICAM1 expression by cell-ELISA	10.1039/C0MD00262C
L1.2	IC₅₀	12 nM Compound: 1	Inhibition of wild type CXCR1 transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs Inhibition of wild type CXCR1 transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs	[PMID: 19560921]
L1.2	IC₅₀	> 10 μM Compound: 1	Inhibition of CXCR1 Lys99Ala mutant transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs Inhibition of CXCR1 Lys99Ala mutant transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs	[PMID: 19560921]
RAW264.7	IC₅₀	10.18 μM Compound: Diclofenac	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA	[PMID: 37611534]
RAW264.7	IC₅₀	10.45 μM Compound: Diclofenac	Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of TNF-alpha production preincubated for 2 hrs followed by LPS addition measured after 20 hrs by ELISA method Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of TNF-alpha production preincubated for 2 hrs followed by LPS addition measured after 20 hrs by ELISA method	[PMID: 37182334]
RAW264.7	IC₅₀	19.59 μM Compound: Diclofenac	Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of IL-6 production preincubated for 2 hrs followed by LPS addition measured after 20 hrs by ELISA method Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of IL-6 production preincubated for 2 hrs followed by LPS addition measured after 20 hrs by ELISA method	[PMID: 37182334]
RAW264.7	IC₅₀	21.34 μM Compound: Diclofenac	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production preincubated for 2 hrs followed by LPS stimulation and measured after 20 hrs by ELISA	[PMID: 37611534]
RAW264.7	IC₅₀	25.34 μM Compound: Diclofenac	Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of NO production preincubated for 2 hrs followed by LPS addition measured after 20 hrs by DAF-FM staining based assay Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of NO production preincubated for 2 hrs followed by LPS addition measured after 20 hrs by DAF-FM staining based assay	[PMID: 37182334]
RAW264.7	IC₅₀	26.26 μM Compound: Diclofenac	Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of ROS production by DCFH-DA staining based assay Antiinflammatory activity in LPS-activated mouse RAW264.7 cells assessed as inhibition of ROS production by DCFH-DA staining based assay	[PMID: 37182334]
RAW264.7	IC₅₀	50.08 μM Compound: Diclofenac	Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced ROS production preincubated with compound for 2 hrs followed by LPS stimulation and measured after 20 hrs by DCFH-DA probe based fluorescence analysis Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced ROS production preincubated with compound for 2 hrs followed by LPS stimulation and measured after 20 hrs by DCFH-DA probe based fluorescence analysis	[PMID: 37611534]
RAW264.7	IC₅₀	54.66 μM Compound: Diclofenac	Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated with compound for 2 hrs followed by LPS stimulation and measured after 20 hrs by fluorescence microscopic analysis Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated with compound for 2 hrs followed by LPS stimulation and measured after 20 hrs by fluorescence microscopic analysis	[PMID: 37611534]
Sf21	IC₅₀	23.62 μM Compound: Diclofenac	Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell	[PMID: 20974503]
Sf9	IC₅₀	0.03 μM Compound: diclofenac	Inhibition of human COX1 expressed in sf9 cells Inhibition of human COX1 expressed in sf9 cells	[PMID: 16252917]
Sf9	IC₅₀	0.07 μM Compound: diclofenac	Inhibition of human COX2 expressed in sf9 cells Inhibition of human COX2 expressed in sf9 cells	[PMID: 16252917]
THP-1	IC₅₀	143 μM Compound: Diclofenac	Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation	[PMID: 30818268]
THP-1	IC₅₀	4.86 μM Compound: Diclofenac	Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages preincubated for 6 hrs followed by PMA stimulation by phase contrast microscopic method Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages preincubated for 6 hrs followed by PMA stimulation by phase contrast microscopic method	[PMID: 29289887]
Ventricular myocyte	IC₅₀	12.89 μM Compound: Diclofenac	Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes	[PMID: 22761000]

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.

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).

Molecular Weight

296.15

Formula

C₁₄H₁₁Cl₂NO₂

CAS No.

15307-86-5

Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (422.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (281 KB) SDS (788 KB)

COA (251 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3767 mL	16.8833 mL	33.7667 mL	84.4167 mL
	5 mM	0.6753 mL	3.3767 mL	6.7533 mL	16.8833 mL
	10 mM	0.3377 mL	1.6883 mL	3.3767 mL	8.4417 mL
	15 mM	0.2251 mL	1.1256 mL	2.2511 mL	5.6278 mL
	20 mM	0.1688 mL	0.8442 mL	1.6883 mL	4.2208 mL
	25 mM	0.1351 mL	0.6753 mL	1.3507 mL	3.3767 mL
	30 mM	0.1126 mL	0.5628 mL	1.1256 mL	2.8139 mL
	40 mM	0.0844 mL	0.4221 mL	0.8442 mL	2.1104 mL
	50 mM	0.0675 mL	0.3377 mL	0.6753 mL	1.6883 mL
	60 mM	0.0563 mL	0.2814 mL	0.5628 mL	1.4069 mL
	80 mM	0.0422 mL	0.2110 mL	0.4221 mL	1.0552 mL
	100 mM	0.0338 mL	0.1688 mL	0.3377 mL	0.8442 mL

Diclofenac Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Diclofenac15307-86-5COXApoptosisCyclooxygenaseanti-inflammatoryCOX-1COX-2CHOovineneuralstemcellsNSCscaspasecascadeInhibitorinhibitorinhibit

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Diclofenac

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Diclofenac Related Antibodies

24 Publications Citing Use of MCE Diclofenac

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