1. Immunology/Inflammation
  2. COX
  3. Diclofenac Sodium

Diclofenac Sodium (Synonyms: GP 45840)

Cat. No.: HY-15037 Purity: >98.0%
Handling Instructions

Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.

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

Diclofenac Sodium Chemical Structure

Diclofenac Sodium Chemical Structure

CAS No. : 15307-79-6

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10 mM * 1 mL in Water USD 66 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
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Based on 5 publication(s) in Google Scholar

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Description

Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.

IC50 & Target

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 Sodium (GP 45840) is a potent COX inhibitor, with IC50s of 4 nM and 1.3 nM for human COX-1 and COX-2 in the CHO cells, respectively. Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7 ± 3 nM[1]. Diclofenac Sodium exihibits inhibition on COX-1 and COX-2 enzyme with IC50s of 5.1 and 0.84 μM, respectively[2].

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) shows anti-inflammatory activity in mice[2]. Diclofenac (10 mg/kg) decreases oxidized low-densitylipoprotein (Ox-LDL), but shows no effects on the kinetics parameters of catalase and glutathione peroxidase via intramuscularly injection into rats[3].

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

H2O : 10 mg/mL (31.43 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1434 mL 15.7168 mL 31.4337 mL
5 mM 0.6287 mL 3.1434 mL 6.2867 mL
10 mM 0.3143 mL 1.5717 mL 3.1434 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
Male Sprague-Dawley rats (150 ± 200 g) are dosed orally with Diclofenac either once (acute dosing) or twice daily for 5 days (chronic dosing). A plasma sample is obtained 1 h after the morning dose on day 4 for measurement of Diclofenac concentration. Immediately after the administration of the last dose on day 5, the rats are injected via a tail vein with 0.5 mL of 51Cr-labelled red blood cells from a donor rat after incubation with sodium 51chromate. The rats are placed individually in metabolism cages with food and water ad libitum. Faeces are collected for a 48 h period and 51Cr faecal excretion is calculated as a % of total injected dose (20 mCi per animal)[1].
Squirrel monkeys[1]
Squirrel monkeys (Saimiri sciureus; 0.8 ± 1.4 kg) are dosed orally with Diclofenac twice daily for 1 ± 5 days. One hour after administration of the last dose, 51CrCl3 in sterile saline (1 mL/kg, 4 ± 5 mCi per animal) is injected via a saphenous vein and plasma samples are obtained for measurement of Diclofenac concentration. The monkeys are then housed individually in metabolism cages. Faeces are collected for a 24 h period and 51Cr faecal excretion is calculated as a % of total injected dose[1].

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

References
Molecular Weight

318.13

Formula

C₁₄H₁₀Cl₂NNaO₂

CAS No.

15307-79-6

SMILES

[O-]C(CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl)=O.[Na+]

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Diclofenac Sodium
Cat. No.:
HY-15037
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Diclofenac Sodium

Cat. No.: HY-15037