Firocoxib is a coxib exhibiting high selectivity to inhibit COX-2. In vitro canine whole blood assays have demonstrated Firocoxib to be 350–430-fold more selective for COX-2 than for COX-1. COX-1 is constitutively expressed and enzymatically active in a variety of sites, including the stomach, intestine, kidneys, and platelets. COX-1 is the isoform largely responsible for the physiologic functions of eicosanoids, including gastric mucosal protection, renal blood flow, and vascular hemostasis. COX-2 expression is primarily induced by mediators such as serum growth factors, cytokines, and mitogens. COX-2 is primarily responsible for the synthesis of eicosanoids associated with inflammation.
| Cell Experiment | |
|---|---|
| Cell lines | isolated peripheral blood mononuclear cells |
| Preparation method | Peripheral blood mononuclear cells were isolated by density gradient centrifugation and incubated at 37°C with medium alone, firocoxib (100 ng/mL), LPS (1 ng/mL or 1 μg/mL), or combinations of firocoxib and both LPS concentrations. After 4 hours, supernatants were collected and tested for prostaglandin E2 (PGE2) concentration with an enzyme inhibition assay, and gene expression in cell lysates was measured with PCR assays. |
| Concentrations | 100 ng/mL |
| Incubation time | 4h |
| Animal Experiment | |
|---|---|
| Animal models | Mouse Model of Incisional Pain by objective measurement of mechanical allodynia and thermal hyperalgesia using von Frey and Hargreaves equipment |
| Formulation | diluted in sterile 0.9% physiologic saline |
| Dosages | 10 or 20 mg/kg |
| Administration | intraperitoneally |
| Molecular Weight | 336.4 |
| Formula | C17H20O5S |
| CAS Number | 189954-96-9 |
| Solubility (25°C) | DMSO ≥ 45 mg/mL |
| Storage | -20°C, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Sarah A Wagner, et al. Pharmacokinetics of oral firocoxib in un-weaned calves
[2] Josh R Donnell, et al. Use of firocoxib for the treatment of equine osteoarthritis
[3] Bachir Latli, et al. Synthesis of stable isotope-labelled firocoxib
| Related COX Products |
|---|
| Oxyphenbutazone
Oxyphenbutazone is an orally active non-selective COX inhibitor. Oxyphenbutazone selectively kills non-replicating Mycobaterium tuberculosis. |
| Birch triterpenes
Birch triterpenes is a cyclooxygenase-2 (COX-2) inhibitor that can be used in studies related to epidermolysis bullosa. |
| Naproxcinod
Naproxcinod is a first-of-its-kind (first-in-class) cyclooxygenase-inhibiting nitric oxide donors (CINODs) with analgesic and anti-inflammatory activity for studies related to osteoarthritis and inflammation. |
| Hamaudol
Hamaudol is a chromone isolated from Saposhnikovia divaricata. |
| (±)-Catechin
(±)-Catechin (rel-Cianidanol) is the racemate of Catechin. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
