1. Loxoprofen sodium

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

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Loxoprofen sodium Chemical Structure

Loxoprofen sodium Chemical Structure

CAS No. : 80382-23-6

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10 mM * 1 mL in DMSO
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Description

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

In Vitro

Loxoprofen sodium, an anti-inflammatory prodrug (NSAID), is a nonselective COX inhibitor with IC50s of 6.5 and 13.5μM for COX-1 and COX-2 in human whole blood assays, respectively[1].
Loxoprofen (LOX) sodium 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 sodium 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.

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

268.28

Formula

C15H17NaO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(CCC1)CC2=CC=C(C(C)C(O[Na])=O)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (372.74 mM; Need ultrasonic)

DMSO : 19.23 mg/mL (71.68 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 3.7274 mL 18.6372 mL 37.2745 mL
5 mM 0.7455 mL 3.7274 mL 7.4549 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.92 mg/mL (7.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.92 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 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: ≥ 1.92 mg/mL (7.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.92 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 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:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.7274 mL 18.6372 mL 37.2745 mL 93.1862 mL
5 mM 0.7455 mL 3.7274 mL 7.4549 mL 18.6372 mL
10 mM 0.3727 mL 1.8637 mL 3.7274 mL 9.3186 mL
15 mM 0.2485 mL 1.2425 mL 2.4850 mL 6.2124 mL
20 mM 0.1864 mL 0.9319 mL 1.8637 mL 4.6593 mL
25 mM 0.1491 mL 0.7455 mL 1.4910 mL 3.7274 mL
30 mM 0.1242 mL 0.6212 mL 1.2425 mL 3.1062 mL
40 mM 0.0932 mL 0.4659 mL 0.9319 mL 2.3297 mL
50 mM 0.0745 mL 0.3727 mL 0.7455 mL 1.8637 mL
60 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5531 mL
H2O 80 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
100 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9319 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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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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Loxoprofen sodium
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