2. Others
  3. Drug Derivative
  4. Ampiroxicam

Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases.

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

Ampiroxicam

Ampiroxicam Chemical Structure

CAS No. : 99464-64-9

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Ampiroxicam:

Ampiroxicam Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases[1][2][3][4].

IC50 & Target

COX

 

Parmacokinetics
Species Dose Route AUC Bioavailability Cmax Tmax
Rat[2] 10 mg/kg p.o. / / 26 μg/mL 4 h
Rat[2] 3.2 mg/kg p.o. 126 μg·h/mL 91 % 12 μg/mL 2 h
Rat[2] 3.2 mg/kg i.v. 125 μg·h/mL 91 % / /
Dog[2] 1.0 mg/kg p.o. 99 μg·h/mL 72 % 2.5 μg/mL 1.5 h
Dog[2] 1.0 mg/kg i.v. 108 μg·h/mL 78 % / /
Monkey[2] 5.0 mg/kg p.o. 207 μg·h/mL 52 % 16 μg/mL 2 h
Monkey[2] 5.0 mg/kg i.v. 280 μg·h/mL 54 % / /
In Vivo

Ampiroxicam (1%; topical occlusive patch; daily for 3 consecutive days; single dose on day 9; single dose on day 21) induces contact hypersensitivity in female Hartley guinea pigs. Sensitized animals show positive responses to UVA-irradiated ampiroxicam and cross-react with thiosalicylates, but do not respond to non-irradiated ampiroxicam or piroxicam[1].
Ampiroxicam (1-4.1 mg/kg; p.o.; single dose) inhibits the stretching response in fasted CF-1 mice induced by benzoquinone, with an MPE50 of 2.0 mg/kg[2].
Ampiroxicam (4.3-41 mg/kg; p.o.; single daily dose for 5 days) inhibits carrageenan-induced hind paw edema in fasted Sprague-Dawley rats[2].

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

Animal Model: Hartley (female, 380-450 g, contact hypersensitivity model via adjuvant patch test modified maximization method)[1]
Dosage: 1% (UVA-irradiated, sensitization); 1% (UVA-irradiated, challenge); 1% (thiosalicylate challenge)
Administration: topical occlusive patch; daily for 3 consecutive days (primary sensitization); topical occlusive patch; single dose on day 9 (repeat sensitization); topical open application; single dose on day 21 (challenge)
Result: Induced a mean total skin reaction score of 3.3 (5/5 animals positive) when challenged with UVA-irradiated 1% ampiroxicam.
Induced a mean total skin reaction score of 4.7 (5/5 animals positive) when challenged with 1% thiosalicylate.
Induced a mean total skin reaction score of 4.0 (4/5 animals positive) with UVA (25.5 J/cm2)-irradiated 1% ampiroxicam challenge.
Showed no positive reactions to non-irradiated 1% ampiroxicam, UVA-irradiated 1% piroxicam, or non-irradiated 1% piroxicam.
Animal Model: CF-1 (fasted overnight, N ≥5/group)[2]
Dosage: 1.0-4.1 mg/kg
Administration: oral gavage; single dose
Result: Determined an MPE50 of 2.0 mg/kg (95% confidence interval 1.0-4.1 mg/kg) for suppression of phenylbenzoquinone-induced stretching.
Animal Model: Sprague-Dawley (fasted, N ≥6/group)[2]
Dosage: 4.3-41 mg/kg
Administration: oral; single dose; oral; daily; 5 days
Result: Determined an ED50 of 28 mg/kg (95% confidence interval 21-41 mg/kg) for single oral dose administration.
Determined an ED50 of 7.8 mg/kg (95% confidence interval 4.3-28 mg/kg) for 5 consecutive daily oral doses.
Molecular Weight

447.46

Formula

C20H21N3O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC(OC(C1=CC=CC=C12)=C(C(NC3=NC=CC=C3)=O)N(C)S2(=O)=O)C)OCC
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 : 50 mg/mL (111.74 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 2.2348 mL 11.1742 mL 22.3484 mL
5 mM 0.4470 mL 2.2348 mL 4.4697 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.

  • 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 (5.59 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.59 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)

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
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
DMSO 1 mM 2.2348 mL 11.1742 mL 22.3484 mL 55.8709 mL
5 mM 0.4470 mL 2.2348 mL 4.4697 mL 11.1742 mL
10 mM 0.2235 mL 1.1174 mL 2.2348 mL 5.5871 mL
15 mM 0.1490 mL 0.7449 mL 1.4899 mL 3.7247 mL
20 mM 0.1117 mL 0.5587 mL 1.1174 mL 2.7935 mL
25 mM 0.0894 mL 0.4470 mL 0.8939 mL 2.2348 mL
30 mM 0.0745 mL 0.3725 mL 0.7449 mL 1.8624 mL
40 mM 0.0559 mL 0.2794 mL 0.5587 mL 1.3968 mL
50 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1174 mL
60 mM 0.0372 mL 0.1862 mL 0.3725 mL 0.9312 mL
80 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6984 mL
100 mM 0.0223 mL 0.1117 mL 0.2235 mL 0.5587 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Ampiroxicam 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:

Ampiroxicam99464-64-9CP 65703CP65703CP-65703Drug DerivativeDrug derivativeNSAID Prodrugphotosensitivityadjuvant-induced arthritisrheumatismosteoarthritisSprague-Dawley ratsfemale Hartley guinea pigs
Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Ampiroxicam
Cat. No.:
HY-17484
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.