Cimicoxib
Based on 1 Customer Validation
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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- Purity: 98.02%
- CAS No.: 265114-23-6
- 화학식: C16H13ClFN3O3S
- 분자량:381.81
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
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COX-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
3.3 μM
Compound: 51f
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In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells
In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells
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[PMID: 12877584] |
Cimicoxib (15 μM; 30 min) undergoes phase 1 metabolism to form demethyl-cimicoxib in feline hepatic microsomes, with CYP2D15 as the primary metabolizing enzyme and CYP3A12 contributing to a lesser extent, and has lower affinity for feline CYP2D15 orthologs than for canine CYP2D15[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | C0 | T1/2 | CLblood | Vss | AUClast | AUCINF_obs | MRTlast | CLrenal | Tmax | Cmax | Vd/F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Dog[2] | 2 mg/kg | i.v. | 1.81 μg/mL | 1.90 h | 0.49 L/h/kg | 1.39 L/kg | 3.96 μg·h/mL | 4.09 μg·h/mL | 2.54 h | 0.51 mL/h/kg | / | / | / |
| Cat[2] | 1 mg/kg | i.v. | 1.62 μg/mL | 5.16 h | 0.13 | 0.90 L/kg | 7.20 μg·h/mL | 7.54 μg·h/mL | 5.67 h | 0.35 mL/h/kg | / | / | / |
| Horse[4] | 2 mg/kg | o.a. | / | 4.12 h | / | / | 1.08 μg/mL·h | / | 7.03 h | / | 3.66 h | 0.12 μg/mL | 10436 mL/kg |
| Horse[4] | 5 mg/kg | o.a. | / | 5.96 h | / | / | 1.49 μg/mL·h | / | 6.85 h | / | 3.25 h | 0.16 μg/mL | 33340 mL/kg |
Cimicoxib (1 mg/kg; i.v.; single slow bolus injection) administered as a single 1 mg/kg i.v. bolus in healthy European crossbreed cats has a total body clearance of 0.13 L/h kg, a terminal half-life of 5.16 h, and 3.32% of the dose is eliminated in urine with conjugated demethyl-cimicoxib representing the majority of urinary metabolites[2].
Cimicoxib (2 mg/kg; p.o., i.v.; single dose) exhibits significant antipyretic, anti-inflammatory, and analgesic efficacy in beagle dogs with kaolin-induced paw inflammation, with EM dogs requiring lower plasma concentrations for half-maximal effects and PM dogs demonstrating longer effect durations[3].
Cimicoxib (2-5 mg/kg; p.o. via nasogastric tube; single dose) produces mean maximal COX-1 inhibition of 62.4% (fasted) and 54.6% (fed), and mean maximal COX-2 inhibition of 72.1% (fasted) and 68.5% (fed) in healthy mares at the 5 mg/kg dose, while the 2 mg/kg dose yields detectable plasma concentrations but no reported specific inhibition values[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:healthy mares (7-12 years old, 430-570 kg)[4]
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Dosage:2 mg/kg; 5 mg/kg
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Administration:p.o. via nasogastric tube; single dose
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Result:Exhibited detectable plasma concentrations for up to 24 hours at 2 mg/kg dose, with no specific inhibition values reported.
Achieved mean maximal TXB2 (COX-1) inhibition of 62.4% in fasted horses and 54.6% in fed horses at 5 mg/kg dose.
Achieved mean maximal PGE2 (COX-2) inhibition of 72.1% in fasted horses and 68.5% in fed horses at 5 mg/kg dose.
Showed TXB2 inhibition peaking at 1 hour and persisting up to 10 hours at 5 mg/kg dose.
Showed PGE2 inhibition gradually increasing to a peak at 10 hours post-administration at 5 mg/kg dose.
Demonstrated no significant differences in inhibition between fasted and fed groups at 5 mg/kg dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 265114-23-6
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Appearance Solid
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분자량 381.81
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화학식 C16H13ClFN3O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(N2C(C3=CC=C(OC)C(F)=C3)=C(Cl)N=C2)C=C1)(N)=O
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Synonyms
UR-8880
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 125 mg/mL (327.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (284 KB)
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SDS (721 KB)
- English - EN (721 KB)
- Français - FR (721 KB)
- Deutsch - DE (721 KB)
- Norwegian - NO (721 KB)
- Español - ES (721 KB)
- Swedish - SV (721 KB)
- Italian - IT (721 KB)
- Korean - KR (721 KB)
- Portuguese - PT (721 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6191 mL | 13.0955 mL | 26.1910 mL | 65.4776 mL |
| 5 mM | 0.5238 mL | 2.6191 mL | 5.2382 mL | 13.0955 mL | |
| 10 mM | 0.2619 mL | 1.3096 mL | 2.6191 mL | 6.5478 mL | |
| 15 mM | 0.1746 mL | 0.8730 mL | 1.7461 mL | 4.3652 mL | |
| 20 mM | 0.1310 mL | 0.6548 mL | 1.3096 mL | 3.2739 mL | |
| 25 mM | 0.1048 mL | 0.5238 mL | 1.0476 mL | 2.6191 mL | |
| 30 mM | 0.0873 mL | 0.4365 mL | 0.8730 mL | 2.1826 mL | |
| 40 mM | 0.0655 mL | 0.3274 mL | 0.6548 mL | 1.6369 mL | |
| 50 mM | 0.0524 mL | 0.2619 mL | 0.5238 mL | 1.3096 mL | |
| 60 mM | 0.0437 mL | 0.2183 mL | 0.4365 mL | 1.0913 mL | |
| 80 mM | 0.0327 mL | 0.1637 mL | 0.3274 mL | 0.8185 mL | |
| 100 mM | 0.0262 mL | 0.1310 mL | 0.2619 mL | 0.6548 mL |
Cimicoxib Related Classifications
HY-100516 Related Classifications
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