265114-23-6
Chemical Structure
Cimicoxib
Synonym(s): UR-8880
- CAS 番号: 265114-23-6
- Formula:C16H13ClFN3O3S
- Molecular Weight:381.81
IUPAC Name: 4-(4-chloro-5-(3-fluoro-4-methoxyphenyl)-1H-imidazol-1-yl)benzenesulfonamide
InChIKey: KYXDNECMRLFQMZ-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(N2C(C3=CC=C(OC)C(F)=C3)=C(Cl)N=C2)C=C1)(N)=O
Biological Activity: Cimicoxib (UR-8880) is an orally active, blood-brain barrier-permeable COX-2 inhibitor that also exerts targeted inhibition on CYP2D15. It has an IC50 of 66 nM against hCOX-2, an IC50 of 1.6 μM against canine CYP2D15, and an IC50 of 0.056 μM against feline CYP2D15. By inhibiting the COX-2 pathway to reduce the production of thromboxane B2 and prostaglandin E2, Cimicoxib exerts antipyretic, anti-inflammatory and analgesic effects. Cimicoxib is metabolized by CYP2D15 to form demethyl-cimicoxib, undergoes glucuronidation via UDP-glucuronosyltransferases, and exhibits biphasic elimination kinetics in beagle dogs. Cimicoxib is widely used in studies of inflammatory diseases, osteoarthritis, and perioperative pain associated with orthopedic or soft tissue surgeries[1][2][3][4].
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Cimicoxib | 98.02% | Cimicoxib (UR-8880) is an orally active, blood-brain barrier-permeable COX-2 inhibitor that also exerts targeted inhibition on CYP2D15. It has an IC50 of 66 nM against hCOX-2, an IC50 of 1.6 μM against canine CYP2D15, and an IC50 of 0.056 μM against feline CYP2D15. By inhibiting the COX-2 pathway to reduce the production of thromboxane B2 and prostaglandin E2, Cimicoxib exerts antipyretic, anti-inflammatory and analgesic effects. Cimicoxib is metabolized by CYP2D15 to form demethyl-cimicoxib, undergoes glucuronidation via UDP-glucuronosyltransferases, and exhibits biphasic elimination kinetics in beagle dogs. Cimicoxib is widely used in studies of inflammatory diseases, osteoarthritis, and perioperative pain associated with orthopedic or soft tissue surgeries. | ||||||||||||||||||||
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Cimicoxib (Standard) | ≥98% | Cimicoxib (Standard) is the analytical standard of Cimicoxib. This product is intended for research and analytical applications. Cimicoxib (UR-8880) is an orally active, blood-brain barrier-permeable COX-2 inhibitor that also exerts targeted inhibition on CYP2D15. It has an IC50 of 66 nM against hCOX-2, an IC50 of 1.6 μM against canine CYP2D15, and an IC50 of 0.056 μM against feline CYP2D15. By inhibiting the COX-2 pathway to reduce the production of thromboxane B2 and prostaglandin E2, Cimicoxib exerts antipyretic, anti-inflammatory and analgesic effects. Cimicoxib is metabolized by CYP2D15 to form demethyl-cimicoxib, undergoes glucuronidation via UDP-glucuronosyltransferases, and exhibits biphasic elimination kinetics in beagle dogs. Cimicoxib is widely used in studies of inflammatory diseases, osteoarthritis, and perioperative pain associated with orthopedic or soft tissue surgeries. | ||||||||||||||||||||
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- [1]. Pawar V G, et al. Synthesis of 1, 5-disubstituted 4-haloimidazoles from α-aminonitriles[J]. Tetrahedron letters, 2006, 47(31): 5451-5453.
- [2]. Schneider M, et al. Comparative pharmacokinetic profile of cimicoxib in dogs and cats after IV administration. Vet J. 2021;270:105625. [Content Brief]
- [3]. Jeunesse EC, et al. Pharmacokinetic/pharmacodynamic modeling for the determination of a cimicoxib dosing regimen in the dog. BMC Vet Res. 2013;9:250. Published 2013 Dec 11. [Content Brief]
- [4]. Kim TW, et al. Evaluation of pharmacokinetic and pharmacodynamic properties of cimicoxib in fasted and fed horses. N Z Vet J. 2015;63(2):92-97. [Content Brief]
Keywords
