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Vedaprofen

Names

[ CAS No. ]:
71109-09-6

[ Name ]:
Vedaprofen

[Synonym ]:
2-(4-cyclohexylnaphthalen-1-yl)propanoic acid
2-(4-cyclohexyl-1-naphthyl)propanoic acid
acide cyclohexyl-4 naphtalene-1-propionique
Vedaprofen
2-(4-cyclohexyl-1-naphthyl)propionic acid
PM-150
vedaprofene
Quadrisol

Biological Activity

[Description]:

Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory drug (NSAID) for serum TxB2 and exudate PGE2 inhibition [1]. Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM[2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Immunology/Inflammation >> COX

[Target]

COX-1


[In Vitro]

Vedaprofen inhibits horse serum TxB2 and horse exudate PGE2 with IC50s of 9±5 and 630±148 ng/mL, respectively[1].Vedaprofen inhibit the E. coli DNA polymerase III β subunit with antibacterial potency[2]. Vedaprofen shows high E. coli SC binding affinity (Ki=131 μM)[2].

[In Vivo]

Pharmacokinetic parameters of vedaprofen in dogs[3]. Intravenous dose (mg/kg) t1/2β (h) AUC0–48 h (h·ng/mL) AUC0–∞ (h·ng/mL) 0.5 16.8±2.2 8612±1135 9518±1223 Oral dose (mg/kg) t1/2β (h) Cmax (ng/mL) tmax (h) AUC0–48 h (h·ng/mL) AUC0–∞ (h·ng/mL) F0–∞ (%) 0.5 12.7±2.1 2739±277 0.63±0.14 7090±1311 7650±1348 86±7

[References]

[1]. P Lees, et al. PK-PD integration and PK-PD modelling of nonsteroidal anti-inflammatory drugs: principles and applications in veterinary pharmacology. J Vet Pharmacol Ther. 2004 Dec;27(6):491-502.

[2]. Zhou Yin,et al. DNA replication is the target for the antibacterial effects of nonsteroidal anti-inflammatory drugs. Chem Biol. 2014 Apr 24;21(4):481-487.

[3]. M Hoeijmakers, et al. The pharmacokinetics of Vedaprofen and its enantiomers in dogs after single and multiple dosing. J Vet Pharmacol Ther. 2005 Jun;28(3):305-12.

Chemical & Physical Properties

[ Density]:
1.132g/cm3

[ Boiling Point ]:
465.9ºC at 760 mmHg

[ Melting Point ]:
150ºC

[ Molecular Formula ]:
C19H22O2

[ Molecular Weight ]:
282.37700

[ Flash Point ]:
362.5ºC

[ Exact Mass ]:
282.16200

[ PSA ]:
37.30000

[ LogP ]:
5.07560

[ Index of Refraction ]:
1.603

[ Storage condition ]:
-20°C Freezer

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Related Compounds