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Diclofenac

Name: Diclofenac
Brand: TargetMol
SKU: T0196
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0196Cas No. 15307-86-5

Alias Voltaren, Diclofenacum

Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.

Diclofenac

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Purity: 99.99%

Catalog No. T0196Alias Voltaren, DiclofenacumCas No. 15307-86-5

Pack Size	Price	USA Warehouse	Global Warehouse
500 mg	$42	In Stock	In Stock
5 g	$51	-	In Stock
10 g	$83	-	In Stock
1 mL x 10 mM (in DMSO)	$46	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.99%

Color:White

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COA LCMS HNMR

Product Introduction

Diclofenac AI Summary

Diclofenac demonstrates significant anti-inflammatory activity in various animal models and bioassays. It effectively reduces carrageenan and adjuvant-induced paw edema in rats (ED50 = 2.0 mg/kg) and inhibits prostaglandin synthesis, suggesting potential analgesic effects. The compound also displays gastrointestinal tolerability with an ulcerogenic dose (UD) of 20.0 mg/kg, though it shows dose-dependent blood loss and lethality at higher doses. It has a moderate calculated partition coefficient (CLogP = 4.066) and permeability properties, indicating challenges in cellular uptake. Additionally, Diclofenac inhibits fibril formation of various TTR variants, particularly showing strong inhibition (72.0%) of L55P TTR fibril formation. The compound binds to TTR variants with dissociation constants ranging from 60.0 nM to 6180.0 nM. It exhibits potent COX inhibition with IC50 values of 5.0 nM for COX-2 and 70.0 nM for COX-1, indicating potential for treating inflammation-related conditions. Metabolically, Diclofenac shows rapid clearance and high intrinsic clearance rates in liver microsomes, suggesting efficient metabolism and elimination. It has a dissociation constant (pKa) of ~4.8 and demonstrates strong plasma protein binding (99.5%). Despite showing moderate permeability with Log Pe,max = -3.7 and varied bioavailability, the compound's pharmacokinetic profile includes significant total and renal clearance, and hepatic clearance activity in human hepatocytes. Overall, Diclofenac is a potent COX inhibitor and anti-inflammatory agent with metabolic attributes that support rapid elimination and high binding affinity, suggesting significant therapeutic potential albeit with gastrointestinal and renal toxicity at higher doses..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.
Targets&IC50	COX-1 (ovine):0.84 μM, COX-1 (ovine):5.1 μM, COX-1 (human, CHO cells):4 nM, COX-2 (human, CHO cells):1.3 nM
Synonyms	Voltaren, Diclofenacum

Chemical Properties

Molecular Weight	296.15
Formula	C₁₄H₁₁Cl₂NO₂
Cas No.	15307-86-5
Smiles	OC(=O)CC1=C(NC2=C(Cl)C=CC=C2Cl)C=CC=C1
Relative Density.	1.431 g/cm3

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 160 mg/mL (540.27 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (13.51 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3767 mL	16.8833 mL	33.7667 mL	168.8334 mL
5 mM	0.6753 mL	3.3767 mL	6.7533 mL	33.7667 mL
10 mM	0.3377 mL	1.6883 mL	3.3767 mL	16.8833 mL
20 mM	0.1688 mL	0.8442 mL	1.6883 mL	8.4417 mL
50 mM	0.0675 mL	0.3377 mL	0.6753 mL	3.3767 mL
100 mM	0.0338 mL	0.1688 mL	0.3377 mL	1.6883 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc