2. Immunology/Inflammation
  3. COX
  4. Loxoprofen

Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity.

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Loxoprofen Chemical Structure

Loxoprofen Chemical Structure

CAS No. : 68767-14-6

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Loxoprofen:

Loxoprofen Related Antibodies

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COX COX-1 COX-2 COX-3

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Description

Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity[1][2][3][4].

IC50 & Target[1]

COX-1

6.5 μM (IC50, in human whole blood)

COX-2

13.5 μM (IC50, in human whole blood)

In Vitro

Loxoprofen, an anti-inflammatory prodrug (NSAID), is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2 in human whole blood assays, respectively[1].
Loxoprofen (LOX) is a non-selective cyclooxygenase inhibitor that is widely used for the reasearch of pain and inflammation caused by chronic and transitory conditions. Its alcoholic metabolites are formed by carbonyl reductase (CR) and they consist of trans-LOX, which is active, and cis-LOX, which is inactive. In addition, LOX can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP)[2].

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

Loxoprofen Related Antibodies
In Vivo

Loxoprofen sodium (4 mg/kg/day; p.o.; 1 or 8 weeks) reduces atherosclerosis in mice by reducing inflammation[3]. Loxoprofen sodium (60 μg/mL; p.o.; 24 days) suppresses mouse tumor growth by inhibiting VEGF[4].

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

Animal Model: ApoE-/- mice (C57BL/6J-Apoetm1Unc) with high-fat diet (0.2% cholesterol, 21% saturated fat) from 8 to 16 weeks of age[3]
Dosage: 4 mg/kg/day in drinking water
Administration: Oral dosing from 8 to 16 weeks of age or from 15 to 16 weeks of age
Result: Inhibited platelet thromboxane production and platelet aggregation. Reduced extent of atherosclerosis. Suppressed the production of PGE2, TxB2 and PGI2.
Animal Model: 6-week-old male C57BL/6 and BDF1 mice, 100 μL suspensions (2 × 106 cells/mL) of LLC cells and KLN205 cells were injected subcutaneously into C57BL/6 and BDF1 mice, respectively[4].
Dosage: 60 μg/mL
Administration: Oral dosing in drinking water, every day for 24 days
Result: Suppressed tumor growth and angiogenesis, suppressed expression of VEGF in mice with LLC tumor, inhibited tubular formation of HUVECs.
Clinical Trial
Molecular Weight

246.30

Formula

C15H18O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(CCC1)CC2=CC=C(C(C)C(O)=O)C=C2
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 (406.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0601 mL 20.3004 mL 40.6009 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 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 (10.15 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 (10.15 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
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 4.0601 mL 20.3004 mL 40.6009 mL 101.5022 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 mL 20.3004 mL
10 mM 0.4060 mL 2.0300 mL 4.0601 mL 10.1502 mL
15 mM 0.2707 mL 1.3534 mL 2.7067 mL 6.7668 mL
20 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0751 mL
25 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0601 mL
30 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3834 mL
40 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5376 mL
50 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0300 mL
60 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
80 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
100 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
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Loxoprofen 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:

Loxoprofen68767-14-6COXCyclooxygenasepaininflammationNSAIDanalgesicHUVECsLLCVEGFatherosclerosisInhibitorinhibitorinhibit

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