| Size | Price | Stock | Qty |
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| 25mg |
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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.
| Targets |
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 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].
Firocoxib was administered orally to six healthy dogs at a dose of 5.3 ± 0.34 mg/kg once daily for 28 days in a randomized crossover study. No adverse clinical effects (vomiting, diarrhea, depression, inappetence, abdominal pain) were observed during the treatment period. [1] Endoscopic evaluation of the gastrointestinal tract before and after 28 days of treatment showed no lesions (grade 0) in any dog treated with firocoxib. [1] No significant changes were observed in complete blood count, serum biochemistry (urea, creatinine, ALT, ALP, GGT), platelet aggregation, buccal mucosal bleeding time, or fecal occult blood tests compared to baseline or control group. [1] Firocoxib did not impair primary hemostasis in healthy dogs, as indicated by unchanged bleeding time and platelet aggregation. [1] |
| 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. Six healthy adult crossbreed dogs (weight 20.2 ± 6.3 kg) were used in a randomized crossover study with a 21-day washout period. Firocoxib was administered orally once daily at a dose of 5.3 ± 0.34 mg/kg for 28 days. The drug was provided as chewable tablets (57 mg or 227 mg) and broken into halves when necessary to achieve the target dose. The control group received lactose (1 mg/kg) orally for 28 days. [1] Blood samples were collected before treatment and on days 7, 14, 21, and 29 for complete blood count, serum biochemistry, platelet aggregation, and buccal mucosal bleeding time measurement. Fecal occult blood tests were performed at the same time points. [1] Gastrointestinal endoscopy was performed under general anesthesia before treatment and on day 29 to assess gastric and duodenal mucosa. Anesthesia was induced with propofol (8–10 mg/kg IV) and maintained with isoflurane in oxygen. Lactated Ringer’s solution was administered intravenously at 5 mL/kg/h during the procedure. [1] Endoscopic lesions were scored from grade 0 (no lesions) to grade 6 (ulcers of any size). [1] |
| Toxicity/Toxicokinetics |
In healthy dogs, no clinically observable adverse reactions were observed after oral administration of 5.3 ± 0.34 mg/kg fenrocoxib once daily for 28 days. [1]
No gastrointestinal lesions were found during or before and after treatment. [1] No significant changes were observed in hematological, biochemical, or hemostatic parameters. [1] One dog showed a transient increase in serum ALT activity on day 28, but a similar increase was observed in one dog in the lactose group, suggesting that the increase was unrelated to the drug. [1] One dog showed a transient increase in serum GGT activity on days 7 and 14, but returned to normal by day 21. [1] Ferrocoxib did not affect platelet aggregation or bleeding time, indicating that it did not impair primary hemostasis. [1] |
| References |
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| Additional Infomation |
Ferocoxib is an enol ether, a cyclopropylmethyl ether of 3-hydroxy-5,5-dimethyl-4-[4-(methanesulfonyl)phenyl]furan-2-one. It is a selective cyclooxygenase-2 inhibitor used in veterinary medicine to control pain and inflammation associated with osteoarthritis in horses and dogs. It has multiple effects as a nonsteroidal anti-inflammatory drug, a cyclooxygenase-2 inhibitor, an antitumor drug, and a non-narcotic analgesic. It is a butenolide, sulfone, enol ether, and also a cyclopropane compound. Ferocoxib is a selective cyclooxygenase-2 (COX-2) nonsteroidal anti-inflammatory drug. It is currently approved for veterinary use in dogs and horses under the brand names Equioxx and Previcox. Ferocoxib was the first COX-2 inhibitor approved by the U.S. Food and Drug Administration (FDA) for use in horses. Ferocoxib is not approved for use in humans. Drug Indications: For the treatment of pain, inflammation, and fever in horses and dogs.
Relieves pain and inflammation associated with osteoarthritis in horses and reduces associated lameness. Tablets: For relief of pain and inflammation associated with osteoarthritis in dogs. For relief of pain and inflammation following soft tissue, orthopedic, and dental surgery in dogs. Oral paste: For relief of pain and inflammation associated with osteoarthritis in horses and reduces associated lameness. Firocoxib is a selective COX-2 inhibitor developed specifically for veterinary use. [1] It is approved for use in dogs at a dose of 5 mg/kg orally once daily. [1] Clinical studies have shown that firocoxib is effective in controlling pain and inflammation associated with osteoarthritis in dogs. [1] Studies have shown that healthy dogs tolerated firocoxib well after 28 days of administration at the recommended dose, with no gastrointestinal, renal, hepatic, or hemostatic toxicity observed. [1] |
| 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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