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  3. Phenacetin

Phenacetin  (Synonyms: Acetophenetidin)

Cat. No.: HY-B0476 Purity: 99.94%
COA Handling Instructions

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

Phenacetin Chemical Structure

CAS No. : 62-44-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target[1]

COX-3

102 μM (IC50)

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 Cmax (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: T1/2 (2.06 hours), Cmax (6,728.3 μg/L).
Molecular Weight

179.22

Formula

C10H13NO2

CAS No.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
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.
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%

References

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.

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.

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Phenacetin 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.

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