1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Epoxide Hydrolase FLAP
  3. 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.

For research use only. We do not sell to patients.

sEH/FLAP-IN-2

sEH/FLAP-IN-2 Chemical Structure

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Description

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[1].

In Vitro

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.

In Vivo

sEH/FLAP-IN-2 (Compound 6) (10 mg/kg, i.p., once) effectively modulates the lipid mediator profile in a mouse peritonitis model by dually inhibiting FLAP and sEH, shifting the lipid mediator profile from a pro-inflammatory state (LTs and DHETs) to an anti-inflammatory state (EETs)[1].

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.
Molecular Weight

447.57

Formula

C26H33N5O2

SMILES

O=C(NCC1=CC=C(N)C=C1)C2=CC=C(NC(NCC34CC5CC(C4)CC(C5)C3)=O)C=C2N

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
sEH/FLAP-IN-2
Cat. No.:
HY-179441
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