Diclofenac diethylamine

SKU: orb1224009

Description

Diclofenac Diethylamine is a non-selective COX inhibitor used as a nonsteroidal anti-inflammatory drug (NSAID).(In Vitro):Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7±3 nM.Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner.Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3.(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.Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 78213-16-8
• MW: 369.29
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₂Cl₂N₂O₂
• SMILES: CCNCC.OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
• Target: Others
• Solubility: Ethanol: 74 mg/mL (200.38 mM); DMSO: 74 mg/mL (200.38 mM)

Bioactivity

• 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. Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows In vivo anti-inflammatory activity in Wistar rats. Animal model: Male Sprague-Dawley rats (150±200 g). 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. 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).
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• In Vitro:
  Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7±3 nM. Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner. Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3. Cell Viability Assay 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. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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Gene Symbol

Others