sEH/FLAP-IN-2
sEH/FLAP-IN-2 is a selective sEH (IC50 = 12.6 nM)/FLAP dual inhibitor. sEH/FLAP-IN-2 highlights the reduction of 5-LOX/FLAP- and sEH-derived LMs, resulting in a favourable redistribution of LMs. sEH/FLAP-IN-2 can be used for the study of peritonitis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C26H33N5O2
- Masse moléculaire:447.57
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
sEH/FLAP-IN-2 (Compound 6) shows no significant inhibitory activity against 5-LOX, with an IC50 value >10 μM[1].
sEH/FLAP-IN-2 (10 μM, 15 min) significantly inhibits the formation of 5-LOX products (LTB4, trans-LTB4, and 5-HETE) in the FLAP-dependent system without exogenous arachidonic acid (AA) in human neutrophils, with a residual activity of 35.7%; in the presence of exogenous AA, its inhibitory activity was weakened (IC50 > 10 μM)[1].
sEH/FLAP-IN-2 (0.1-10 μM, 16 min) has no significant effect on the activities of COX-1, COX-2, and mPGES-1[1].
sEH/FLAP-IN-2 (0.1-10 μM, 120 min) concentration-dependently inhibits 5-LOX/FLAP-derived mediators (such as LTB4 and LTC4), especially in M1-MDM; simultaneously, it increases COX-derived prostaglandins (such as PGE2 and PGD2) but does not affect SPM (such as RvD5) levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CD-1 mice (33-39 g, 8 weeks old) were given an acute inflammatory response via intraperitoneal injection of Zymosan (HY-159069) (1 mg/mouse)[1].
-
Dosage:10 mg/kg
-
Administration:I.p., once, 30 mins before zymosan
-
Result:Significantly reduced zymosan-induced levels of pro-inflammatory mediators, including LTB4, 5-HETE, and LTE4.
Increased levels of anti-inflammatory EETs (particularly 11,12-EET and 14,15-EET) while decreasing levels of pro-inflammatory DHETs (such as 11,12-DHET), resulting in an elevated EET/DHET ratio.
PGE2 levels were significantly reduced, but TXB2 was unaffected.
Chemical Information
-
Masse moléculaire 447.57
-
Formule C26H33N5O2
-
SMILES
O=C(NCC1=CC=C(N)C=C1)C2=CC=C(NC(NCC34CC5CC(C4)CC(C5)C3)=O)C=C2N
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Ciaglia T, et al. An adamantylureido-benzylamide aniline as FLAP/sEH dual inhibitor: Rational design, in vitro and in vivo lipidomic profiling. Eur J Med Chem. 2026 Jan 15;302(Pt 2):118338. [Content Brief]
[2]. Yang DM, et al. Discovery of novel indoline derivatives as potent small molecule PD-L1 inhibitors. Bioorg Med Chem Lett. 2026 Feb 1;131:130458. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz