sEH/AChE-IN-5
sEH/AChE-IN-5 is a selective, orally active and brain-penetrant acetylcholinesterase (AChE) and soluble epoxide hydrolase (sEH) dual inhibitor with IC50 values of 1.7 nM and 0.7 nM. sEH/AChE-IN-5 mediates neuroprotection and anti-inflammation via reduced TNF-α, IL-1β, IL-6, iNOS. sEH/AChE-IN-5 improves Scopolamine (HY-N0296)-induced learning and memory deficits mice. sEH/AChE-IN-5 can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C34H29ClF3N7O2
- Molecular Weight:660.09
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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AChE 1.7 nM (IC50) |
sEH 0.7 nM (IC50) |
IL-1β |
IL-6 |
sEH/AChE-IN-5 (Compound z43) potently inhibits recombinant hAChE with an IC50 of 1.7 nM and inhibits hBuChE with an IC50 of 942.0 nM[1].
sEH/AChE-IN-5 potently inhibits recombinant hsEH with an IC50 of 0.7 nM[1].
sEH/AChE-IN-5 (20 μM; 48 h) exhibits low cytotoxicity in HepG2, SMMC7721, and SH-SY5Y cell lines, with IC50 values of 82.27 μM, >100 μM, and >20 μM respectively[1].
sEH/AChE-IN-5 (1.25-20 μM) exhibits no significant cytotoxicity in PC12 and BV-2 cell lines at concentrations up to 20 μM[1].
sEH/AChE-IN-5 (5-20 μM; 26 h) protects PC12 cells from H2O2-induced toxicity, increasing cell viability by over 20% at 5 μM in a dose-dependent manner[1].
sEH/AChE-IN-5 (5-20 μM; 1 h pretreatment) dose-dependently reduces LPS (HY-D1056)-induced TNF-α, IL-1β, IL-6, and iNOS levels in BV-2 cells, restoring inflammatory factor levels to near normal at 20 μM[1].
sEH/AChE-IN-5 does not inhibit CYP1A2, shows moderate inhibition of CYP2C9, CYP2C19, and CYP2D6, strongly inhibits CYP3A4 (IC50 = 0.324 μM), and exhibits high BBB permeability via PAMPA (Pe = 3.33 × 10-6 cm/s)[1].
sEH/AChE-IN-5 shows high plasma protein binding in human, dog plasma, with over 99.9% bound in all tested species[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV-2 cells
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Concentration:5, 10, 20 μM
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Incubation Time:1 h pretreatment before LPS
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Result:Does-dependently reduces LPS-induced TNF-α, IL-1β, IL-6.
Restored inflammatory factor levels to near normal at 20 μM.
sEH/AChE-IN-5 (30-1200 mg/kg; i.g.) exhibits favorable acute safety in female Kunming mice, with no observed organ toxicity or adverse events[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Alzheimer's disease ICR mice (male, 3-4 weeks old, 18-22 g, Scopolamine-induced cognitive impairment)[1]
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Dosage:5 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:I.g.; daily; 11 days
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Result:Increased Scopolamine-reduced spontaneous alternation rate from 42.28% to 55.93% (5 mg/kg), 56.79% (10 mg/kg), and 59.35% (30 mg/kg) in the Y-maze test.
Maintained stable total arm entries across all groups, indicating no motor impairment.
Increased Scopolamine-reduced discrimination index from 11.80% to 21.62% (5 mg/kg), 23.82% (10 mg/kg), and 27.99% (30 mg/kg) in the novel object recognition test.
Reversed Scopolamine-elevated brain acetylcholinesterase activity in a dose-dependent manner.
Chemical Information
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Molecular Weight 660.09
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Formula C34H29ClF3N7O2
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SMILES
O=C(NCC1=CC=C(C#N)C=C1C(F)(F)F)C2=CC=CC(OCC3=CN(CCNC4=C(CCCC5)C5=NC6=CC(Cl)=CC=C64)N=N3)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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