1. Immunology/Inflammation
    Apoptosis
  2. COX
    Apoptosis
  3. Diclofenac diethylamine

Diclofenac diethylamine 

Cat. No.: HY-15036A Purity: 99.93%
Handling Instructions

Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

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

Diclofenac diethylamine Chemical Structure

Diclofenac diethylamine Chemical Structure

CAS No. : 78213-16-8

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Based on 6 publication(s) in Google Scholar

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Description

Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells[1], and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively[2]. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade[3].

IC50 & Target[1][2]

Human COX-2

1.3 nM (IC50, in CHO cells)

Human COX-1

4 nM (IC50, in CHO cells)

Ovine COX-2

0.84 μM (IC50)

Ovine COX-1

5.1 μM (IC50)

In Vitro

Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7±3 nM[1].
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner[3].
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3[3].

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

Cell Viability Assay[3]

Cell Line: Neural stem cells (NSCs)
Concentration: 1, 3, 10, 30, 60 μM
Incubation Time: 1 day
Result: Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM.

Western Blot Analysis[3]

Cell Line: Neural stem cells (NSCs)
Concentration: 10, 30 or 60 μM
Incubation Time: 6 hours
Result: The activation of caspase-3 was increased in a concentration-dependent manner.
In Vivo

Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days[1].
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats[1].

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

Animal Model: Male Sprague-Dawley rats (150±200 g)[1]
Dosage: 3 mg/kg
Administration: Oral administration, b.i.d., for 5 days
Result: Resulted in a significant increase in faecal 51Cr excretion.
Animal Model: Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2]
Dosage: 10 mg/kg
Administration: Administered via oral route just prior to induction of inflammation
Result: Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h).
Clinical Trial
Molecular Weight

369.29

Formula

C₁₈H₂₂Cl₂N₂O₂

CAS No.

78213-16-8

SMILES

O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl.CCNCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (406.18 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7079 mL 13.5395 mL 27.0790 mL
5 mM 0.5416 mL 2.7079 mL 5.4158 mL
10 mM 0.2708 mL 1.3539 mL 2.7079 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: ≥ 2.5 mg/mL (6.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.93%

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Keywords:

DiclofenacCOXApoptosisCyclooxygenaseanti-inflammatoryCOX-1COX-2CHOovineneuralstemcellsNSCscaspasecascadeInhibitorinhibitorinhibit

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Diclofenac diethylamine
Cat. No.:
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