Firocoxib (Synonyms: ML-1785713) |
Catalog No.GC12397
One-Click Copy Product Info
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COX2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 189954-96-9
Sample solution is provided at 25 µL, 10mM.
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Firocoxib(ML 1785713) is a potent and selective cyclooxygenase (COX)-2 inhibitor with IC50 of 0.13 uM, 58 fold sensitivity for COX2 VSCOX1.IC50 value: 0.13 uM [1]Target: COX2 inhibitorin vitro: Blood concentrations resulting in 50% inhibition of COX-1 and COX-2 activity in vitro were 75 +/- 2 microM and 0.13 +/- 0.03 microM, respectively, and selectivity for inhibiting COX-2 relative to COX-1 was 58. Firocoxib had 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]. in vivo: Administration of firocoxib did not cause any adverse effects on GI, or hematological or serum biochemical variables and appears to have been well tolerated by dogs [2]. Firocoxib (0.5 mg/kg) was initially administered i.v. to calves, and following a 14-day washout period, animals received firocoxib orally prior to cautery dehorning. Firocoxib concentrations were determined by liquid chromatography-tandem mass spectrometry [3]. Firocoxib 5 mg/kg was given orally once daily for 180 days to five dogs with clinical signs and histopathological lesions consistent with solar dermatitis/actinic keratosis. On days 0, 50 and 180, the severity of erythema, skin shine, induration and the number of comedones were evaluated by a clinical scoring system [4].
References:
[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.
[2]. 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.
[3]. 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.
[4]. 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.
| Cas No. | 189954-96-9 | SDF | |
| Synonyms | ML-1785713 | ||
| Chemical Name | 3-(cyclopropylmethoxy)-5,5-dimethyl-4-(4-methylsulfonylphenyl)furan-2-one | ||
| Canonical SMILES | CC1(C(=C(C(=O)O1)OCC2CC2)C3=CC=C(C=C3)S(=O)(=O)C)C | ||
| Formula | C17H20O5S | M.Wt | 336.4 |
| Solubility | DMF: 3mg/mL,DMSO: 3mg/mL,DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9727 mL | 14.8633 mL | 29.7265 mL |
| 5 mM | 594.5 μL | 2.9727 mL | 5.9453 mL |
| 10 mM | 297.3 μL | 1.4863 mL | 2.9727 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)