Phenacetin (Synonyms: Acetophenetidin)

Name: Phenacetin
Brand: MedChemExpress
SKU: HY-B0476
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0476 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats.

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

Phenacetin Chemical Structure

CAS No. : 62-44-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
1 g	USD 66	In-stock	Estimated Time of Arrival: December 31
5 g	USD 106	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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View All Isoforms

COX COX-1 COX-2 COX-3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

COX-3

102 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 500 μM Compound: phenacetin	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]

In Vitro

Phenacetin shows inhibitory activity for COX-3 with an IC₅₀ value of 102 μM in insect cells ^[1].
Phenacetin is a substrate widely used as an in vitro and in vivo probe to measure the activity of CYP1A2, because the metabolism of phenacetin to acetaminophen is thought to be a selective CYP1A2-mediated reaction^[2]^[3].

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

In Vivo

Phenacetin exhibits elimination half-life (rat 2.06 h) and C_max (6,728.3 μg/L) following oral administration (rat 20 mg/kg)^[2].

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

Animal Model:	Male Sprague-Dawley rats (180-200 g)^[2]
Dosage:	20 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	T_1/2 (2.06 hours), C_max (6,728.3 μg/L).

Molecular Weight

179.22

Formula

C₁₀H₁₃NO₂

CAS No.

62-44-2

Appearance

Solid

Color

White to off-white

SMILES

CC(NC1=CC=C(OCC)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (557.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 0.67 mg/mL (3.74 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.5797 mL	27.8987 mL	55.7973 mL
5 mM	1.1159 mL	5.5797 mL	11.1595 mL
10 mM	0.5580 mL	2.7899 mL	5.5797 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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.

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: ≥ 2.5 mg/mL (13.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (13.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (13.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

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: 99.94%

Select Batch:

Data Sheet (272 KB) SDS (419 KB)

COA (244 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Chandrasekharan NV, et al. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: cloning, structure, and expression. Proc Natl Acad Sci U S A. 2002 Oct 15;99(21):13926-31. [Content Brief]

[2]. Xiao-Meng He, et al. Effects of long-term smoking on the activity and mRNA expression of CYP isozymes in rats. J Thorac Dis. 2015 Oct; 7(10): 1725–1731. [Content Brief]

[3]. Na Gao, et al. Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats. PLoS One. 2014; 9(2): e89752. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	5.5797 mL	27.8987 mL	55.7973 mL	139.4934 mL
DMSO	5 mM	1.1159 mL	5.5797 mL	11.1595 mL	27.8987 mL
	10 mM	0.5580 mL	2.7899 mL	5.5797 mL	13.9493 mL
	15 mM	0.3720 mL	1.8599 mL	3.7198 mL	9.2996 mL
	20 mM	0.2790 mL	1.3949 mL	2.7899 mL	6.9747 mL
	25 mM	0.2232 mL	1.1159 mL	2.2319 mL	5.5797 mL
	30 mM	0.1860 mL	0.9300 mL	1.8599 mL	4.6498 mL
	40 mM	0.1395 mL	0.6975 mL	1.3949 mL	3.4873 mL
	50 mM	0.1116 mL	0.5580 mL	1.1159 mL	2.7899 mL
	60 mM	0.0930 mL	0.4650 mL	0.9300 mL	2.3249 mL
	80 mM	0.0697 mL	0.3487 mL	0.6975 mL	1.7437 mL
	100 mM	0.0558 mL	0.2790 mL	0.5580 mL	1.3949 mL

* 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.

Phenacetin Related Classifications

Inflammation/Immunology

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:

Phenacetin62-44-2AcetophenetidinCOXCyclooxygenaseanalgesicantipyreticCOX-3CYP1A2probeInhibitorinhibitorinhibit

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Phenacetin (Synonyms: Acetophenetidin)

Customer Review

Other Forms of Phenacetin:

Phenacetin Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All COX Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Phenacetin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Phenacetin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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