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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 |
[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 |
|---|
| Sudoxicam
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory agent from the enol-carboxamide class. |
| Metyrosine
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine significantly inhibits high COX-2 activity. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. |
| PPOH
PPOH, a fatty acid derivative, is a selective cyclooxygenase (COX) inhibitor that inhibits arachidonic acid cyclooxygenase activity in renal cortical microsomes. |
| Tenidap
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. |
| COX-2-IN-6
COX-2-IN-6 is an orally active, gut-restricted and selective cyclooxygenase-2 (COX-2) inhibitor for colorectal Chemoprevention of cancer. |
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