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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.02%
- CAS 番号: 265114-23-6
- 分子式: C16H13ClFN3O3S
- 分子量:381.81
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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 |
化学情報
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CAS 番号 265114-23-6
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性状 Solid
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分子量 381.81
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分子式 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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別名
UR-8880
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (284 KB)
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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-100516 関連分類
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