| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Firocoxib (formerly ML-1785713; ML1785713) is a novel, potent and selective cyclooxygenase (COX)-2 inhibitor (IC50 = 0.13 uM) with 58-fold sensitivity for COX2 over COX1. It is a non-steroidal anti-inflammatory drugs (NSAIDs) of the COX-2 inhibitor class, the conversion of arachidonic acid into prostaglandin is catalysed by the cyclo-oxygenases (COX-1/COX-2). Several studies indicate that COX-2 is overexpressed in actinic keratosis in humans and dogs. Firocoxib is a COX-2-selective inhibitor that blocks the biochemical activity of COX-2.
| ln Vitro |
The IC50 values of COX-1 and COX-2 are typically compared in order to calculate the COX-1:COX-2 selectivity ratio. Compared to IC50 values, IC80 values are more indicative of steady-state plasma drug concentrations [1]. Based on the IC80 value, the selectivity ratio of firocoxib was 121 (the IC80 values for COX-2 and COX-1 were 0.36 μM and 43.6 μM, respectively). This suggests that COX-2 selectivity remains constant at concentrations higher than the IC50. Interestingly, doses of firocoxib that inhibit COX-2 by 80% to 95% also inhibit COX-1 by less than 20% [1].
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| ln Vivo |
Giving firocoxib to female domestic shorthair cats orally, either one or fourteen hours prior to an LPS challenge, effectively lowers their fever [1]. Male cats were used to test the pharmacokinetic characteristics of firocoxib following oral (3 mg/kg) and intravenous (2 mg/kg) administration. Firocoxib has an elimination half-life of 8.7 to 12.2 hours, a low plasma clearance of 4.7 to 5.8 mL/min/kg, and a moderate to high oral bioavailability of 54% to 70% [1].
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| Animal Protocol |
Animal/Disease Models: 14 healthy female domestic shorthair cats (11-15 months old, 2.9-3.9 kg), lipopolysaccharide (LPS) [1]
Doses: 0.75 mg/kg, 1.5 mg/kg Route of Administration: po (oral gavage) Experimental Results: Effective attenuation of febrile symptoms in cats when administered 1 or 14 hrs (hrs (hours)) before LPS challenge. |
| References |
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| Additional Infomation |
Firocoxib is an enol ether that is the cyclopropylmethyl ether of 3-hydroxy-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2-one. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in horses and dogs. It has a role as a non-steroidal anti-inflammatory drug, a cyclooxygenase 2 inhibitor, an antineoplastic agent and a non-narcotic analgesic. It is a butenolide, a sulfone, an enol ether and a member of cyclopropanes.
Firocoxib is a cycooxygenase-2 (COX-2) selective non-steroidal anti-inflammatory drug. It currently approved for veterinary use in dogs and horses under the brand names Equioxx and Previcox. Firocoxib was the first COX-2 inhibitor approved by the U.S. Food and Drug Administration for horses. Firocoxib is not intended or approved for use in human medicine. Drug Indication Used for the treatment of pain inflammation and fever in horses and dogs. Alleviation of pain and inflammation associated with osteoarthritis and reduction of associated lameness in horses. TabletsFor the relief of pain and inflammation associated with osteoarthritis in dogs. For the relief of postoperative pain and inflammation associated with soft-tissue, orthopaedic and dental surgery in dogs. Oral pasteAlleviation of pain and inflammation associated with osteoarthritis and reduction of associated lameness in horses. |
| Molecular Formula |
C17H20O5S
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| Molecular Weight |
336.4
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| Exact Mass |
336.103
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| CAS # |
189954-96-9
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| Related CAS # |
Firocoxib-d4;1325700-11-5
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| PubChem CID |
208910
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
563.9±50.0 °C at 760 mmHg
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| Melting Point |
78-80°C
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| Flash Point |
294.8±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.584
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| LogP |
1.23
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
614
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FULAPETWGIGNMT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20O5S/c1-17(2)14(12-6-8-13(9-7-12)23(3,19)20)15(16(18)22-17)21-10-11-4-5-11/h6-9,11H,4-5,10H2,1-3H3
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9727 mL | 14.8633 mL | 29.7265 mL | |
| 5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL | |
| 10 mM | 0.2973 mL | 1.4863 mL | 2.9727 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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