Bioactivity | Floctafenine, a nonsteroidal anti-inflammatory agent (NSAID), acts as an effective analgesic agent[1][2]. Floctafenine is an inhibitor of COX-1 and COX-2 activities in vitro,showing a slightly higher potency towards COX-I. Floctafenine is used for the research of short term pain treatment[3]. |
Invitro | Floctafenine (0.1-100 μM; in the presence of LPS; 24 hours) is slightly more potent 1.5-fold to inhibit in vitro platelet COX-I than monocyte COX-2. The IC50 values for platelet COX-I and monocyte COX-2 inhibition are 2.33 μM (95%CI) and 3.47 μM (95%CI), respectively in heparinized whole blood samples[3].Floctafenine (0.1-100 μM; in the presence of A23187; 1 hour) does not significantly affect A23187-caused LTB4 generation even up to 100 μM[3]. |
In Vivo | Floctafenine (intraperitoneal injection; 50 mg/kg; single dose; 30 minutes prior to p-benzoquinone) has an inhibitory effects on p-benoquinone-induced writhing in rats, inhibition of writhing is 65.98%[1]. |
Name | Floctafenine |
CAS | 23779-99-9 |
Formula | C20H17F3N2O4 |
Molar Mass | 406.36 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. P Giuseppe, et al. Floctafenine: a valid alternative in patients with adverse reactions to nonsteroidal anti-inflammatory drugs. Ann Allergy Asthma Immunol. 1997 Jan;78(1):74-8. [2]. Gehan Hegazy Hegazy, et al. Synthesis of some floctafenine derivatives of expected anti-inflammatory/analgesic activity. Arch Pharm (Weinheim). 2005 Aug;338(8):378-84. [3]. R Maenthaisong, et al. Clinical pharmacology of cyclooxygenase inhibition and pharmacodynamic interaction with aspirin by floctafenine in Thai healthy subjects.Int J Immunopathol Pharmacol. Apr-Jun 2013;26(2):403-17. |