Firocoxib
Based on 1 Customer Validation
Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.54%
- CAS. Nr.: 189954-96-9
- Formel: C17H20O5S
- Molecular Weight:336.40
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Speicherung:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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COX-2 0.13 μM (IC50) |
COX-1 7.5 μM (IC50) |
The COX-1:COX-2 selectivity ratios generally are established by comparing the IC50 for COX-1 to the IC50 for COX-2. The IC80 value more closely resembles the steady-state plasma drug concentration than does the IC50 value[1].The selectivity ratio for Firocoxib based on the IC80 values is 121 (IC80 of 0.36 μM and 43.6 μM for COX-2 and COX-1, respectively), indicating that selectivity for COX-2 is not reduced at concentrations higher than the IC50. Notably, Firocoxib concentrations that yield 80% to 95% inhibition of COX-2 produce < 20% inhibition of COX-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic properties of Firocoxib are determined after i.v. (2 mg/kg) and oral (3 mg/kg) administration in male cats. Firocoxib has moderate to high oral bioavailability (54% to 70%), low plasma clearance (4.7 to 5.8 mL/min/kg), and an elimination half-life of 8.7 to 12.2 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:14 healthy female domestic shorthair cats (11-15 months old, 2.9-3.9 kg) with lipopolysaccharide (LPS)[1]
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Dosage:0.75 mg/kg, 1.5 mg/kg
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Administration:Oral gavage
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Result:Was efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge.
Chemical Information
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CAS. Nr. 189954-96-9
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Appearance Solid
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Molecular Weight 336.40
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Formel C17H20O5S
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Color White to off-white
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SMILES
O=C1OC(C)(C)C(C2=CC=C(S(=O)(C)=O)C=C2)=C1OCC3CC3
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Synonyms
ML 1785713
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Lösungsmittel & Löslichkeit
DMSO : ≥ 52 mg/mL (154.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Steagall PV, et al. Evaluation of the adverse effects of oral firocoxib in healthy dogs. J Vet Pharmacol Ther. 2007 Jun;30(3):218-23. [Content Brief]
[2]. Stock ML, et al. Pharmacokinetics of firocoxib in preweaned calves after oral and intravenous administration. J Vet Pharmacol Ther. 2014 Oct;37(5):457-63. [Content Brief]
[3]. Albanese F, et al. Clinical outcome and cyclo-oxygenase-2 expression in five dogs with solar dermatitis/actinic keratosis treated with firocoxib. Vet Dermatol. 2013 Dec;24(6):606-12, e147. [Content Brief]
[4]. [1].McCann ME, et al. In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in cats with lipopolysaccharide-induced pyrexia. Am J Vet Res. 2005 Jul;66(7):1278-84. [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 (protect from light, stored under nitrogen). 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 | 2.9727 mL | 14.8633 mL | 29.7265 mL | 74.3163 mL |
| 5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL | 14.8633 mL | |
| 10 mM | 0.2973 mL | 1.4863 mL | 2.9727 mL | 7.4316 mL | |
| 15 mM | 0.1982 mL | 0.9909 mL | 1.9818 mL | 4.9544 mL | |
| 20 mM | 0.1486 mL | 0.7432 mL | 1.4863 mL | 3.7158 mL | |
| 25 mM | 0.1189 mL | 0.5945 mL | 1.1891 mL | 2.9727 mL | |
| 30 mM | 0.0991 mL | 0.4954 mL | 0.9909 mL | 2.4772 mL | |
| 40 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8579 mL | |
| 50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
| 60 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2386 mL | |
| 80 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
| 100 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL |
Firocoxib Related Classifications
HY-14670 Related Classifications
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