1. Immunology/Inflammation
  2. COX
  3. Loxoprofen sodium

Loxoprofen sodium 

Cat. No.: HY-B0578A Purity: ≥98.0%
Handling Instructions

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.

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

Loxoprofen sodium Chemical Structure

Loxoprofen sodium Chemical Structure

CAS No. : 80382-23-6

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

COX-1

6.5 μM (IC50)

COX-2

13.5 μM (IC50)

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].

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].

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.
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: 

DMSO : 19.23 mg/mL (71.68 mM; Need ultrasonic)

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
10 mM 0.3727 mL 1.8637 mL 3.7274 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Loxoprofen sodium
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