15307-81-0

15307-81-0 structure

Name: Diclofenac potassium
Chemical Name: diclofenac potassium
CAS Number: 15307-81-0
Molecular Formula: C₁₄H₁₀Cl₂KNO₂
Molecular Weight: 334.239
Catalog: API Antipyretic analgesics Non-steroidal anti-inflammatory drugs
Create Date: 2018-08-11 17:45:52
Modify Date: 2024-01-02 20:35:00
Diclofenac potassium 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 potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade[3].

Name	diclofenac potassium
Synonyms	Diclofenic potassium Potassium {2-[(2,6-dichlorophenyl)amino]phenyl}acetate Benzeneacetic acid, 2-[(2,6-dichlorophenyl)amino]-, potassium salt (1:1) potassium 2-(2-(2,6-dichlorophenylamino)phenyl)acetate 2-((2,6-Dichlorophenyl)amino)benzeneacetic Acid Monopotassium Salt Diclofenac potassium 2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid, potassium salt Potassium [2-[(2,6-dichlorophenyl)amino]phenyl]acetate UNII-L4D5UA6CB4 MFCD00082254 Cataflam CGP 45840B CGP-45840B 2-[(2,6-Dichlorophenyl)amino]benzeneacetic acid potassium salt, Diclofenac potassium salt

Description	Diclofenac potassium 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 potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade[3].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Inflammation/Immunology Signaling Pathways >> Immunology/Inflammation >> COX
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 nM (IC50) Ovine COX-1:5.1 nM (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]. 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]. 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).
References	[1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17. [2]. Labib MB, et al. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80. [3]. Chiho Kudo, et al. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95.

Boiling Point	412ºC at 760 mmHg
Melting Point	156-158ºC
Molecular Formula	C₁₄H₁₀Cl₂KNO₂
Molecular Weight	334.239
Flash Point	203ºC
Exact Mass	332.972565
PSA	52.16000
LogP	3.10240
Vapour Pressure	1.59E-07mmHg at 25°C

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H302-H411
Precautionary Statements	P301 + P312 + P330
Hazard Codes	T: Toxic;
Risk Phrases	22-51/53
Safety Phrases	61
RIDADR	2811.0
HS Code	2922499990

HS Code	2922499990
Summary	HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

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