Floctafenine
Based on 1 Customer Validation
Floctafenine, a nonsteroidal anti-inflammatory agent (NSAID), acts as an effective analgesic agent. 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 research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 95.28%
- CAS. Nr.: 23779-99-9
- Formel: C20H17F3N2O4
- Molecular Weight:406.36
-
Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
COX-1 |
COX-2 |
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 23779-99-9
-
Appearance Solid
-
Molecular Weight 406.36
-
Formel C20H17F3N2O4
-
Color White to off-white
-
SMILES
O=C(OCC(O)CO)C1=CC=CC=C1NC2=CC=NC3=C(C(F)(F)F)C=CC=C23
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (246.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Reinheit & Dokumentation
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4609 mL | 12.3044 mL | 24.6087 mL | 61.5218 mL |
| 5 mM | 0.4922 mL | 2.4609 mL | 4.9217 mL | 12.3044 mL | |
| 10 mM | 0.2461 mL | 1.2304 mL | 2.4609 mL | 6.1522 mL | |
| 15 mM | 0.1641 mL | 0.8203 mL | 1.6406 mL | 4.1015 mL | |
| 20 mM | 0.1230 mL | 0.6152 mL | 1.2304 mL | 3.0761 mL | |
| 25 mM | 0.0984 mL | 0.4922 mL | 0.9843 mL | 2.4609 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8203 mL | 2.0507 mL | |
| 40 mM | 0.0615 mL | 0.3076 mL | 0.6152 mL | 1.5380 mL | |
| 50 mM | 0.0492 mL | 0.2461 mL | 0.4922 mL | 1.2304 mL | |
| 60 mM | 0.0410 mL | 0.2051 mL | 0.4101 mL | 1.0254 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3076 mL | 0.7690 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2461 mL | 0.6152 mL |