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Amfenac Sodium Monohydrate COX inhibitor

Name: Amfenac Sodium Monohydrate
Brand: Selleck Chemicals
SKU: S4149
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4149

Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively.

Chemical Structure

Molecular Weight: 295.27

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Quality Control

Batch: S414901 DMSO]59 mg/mL]false]Water]59 mg/mL]false]Ethanol]4 mg/mL]false Purity: 99.94%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.94

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other COX Inhibitors	NS-398 (NS398) Paeoniflorin (NSC 178886) Lumiracoxib Xanthohumol Bufexamac Nimesulide Ginsenoside Rd Oroxin B Phenacetin Tolfenamic Acid

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (199.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 59 mg/mL

Ethanol : 4 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.45mg/ml (8.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 49 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.35mg/ml (1.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	295.27	Formula	C₁₅H₁₂NO₃.H₂O.Na	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	61618-27-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)C(=O)C2=CC=CC(=C2N)CC(=O)[O-].O.[Na+]

Mechanism of Action

Targets/IC₅₀/Ki	COX-2 150 nM COX-1 250 nM
In vitro	Amfenac is a potent inhibitor of both COX-1 and COX-2 with IC50 of 0.25 and 0.15 μM.
In vivo	Amfenac possesses both antipyretic and analgesic properties in vivo. Amfenac (4 mg/kg) suppressed acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation by 33% and 28%, respectively, which is 16.4 and 22.8 times more potent than phenylbutazone. The analgesic activity of Amfenac is 43 times that of acetylsalicylic acid in the Randall-Selitto assay, and 156 and 56.3 times more potent than phenylbutazone in the acetylcholine-induced abdominal constriction in mice and in the bradykinin-induced nociceptive response in dogs, respectively. Amfenac produces less gastric irritation than acetylsalicylic acid when applied topically to the exposed gastric mucosa of cats or when administered orally to rats and dogs. Upon subchronic oral administration to rats, the therapeutic ratio of Amfenac is twice that of phenylbutazone.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10850857/ [2] https://pubmed.ncbi.nlm.nih.gov/871089/

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