2. Neuronal Signaling Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Cholinesterase (ChE) Epoxide Hydrolase TNF Receptor Interleukin Related
  4. 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.

sEH/AChE-IN-5

sEH/AChE-IN-5 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

sEH/AChE-IN-5 Related Antibodies

Top Publications Citing Use of Products

View All Cholinesterase (ChE) Isoform Specific Products:

View All Isoforms
AChE BChE

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

AChE

1.7 nM (IC50)

sEH

0.7 nM (IC50)

IL-1β

 

IL-6

 

In Vitro

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.

sEH/AChE-IN-5 Related Antibodies

ELISA Assay[1]

Cell Line: BV-2 cells
Concentration: 5, 10, 20 μM
Incubation Time: 1 h pretreatment before LPS
Result: Does-dependently reduces LPS-induced TNF-α, IL-1β, IL-6.
Restored inflammatory factor levels to near normal at 20 μM.
In Vivo

sEH/AChE-IN-5 (Compound z43) (5-30 mg/kg; i.g.; daily 11 days) dose-dependently improves Scopolamine (HY-N0296)-induced learning and memory deficits in male ICR mice[1].
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.

Animal Model: Alzheimer's disease ICR mice (male, 3-4 weeks old, 18-22 g, Scopolamine-induced cognitive impairment)[1]
Dosage: 5 mg/kg; 10 mg/kg; 30 mg/kg
Administration: I.g.; daily; 11 days
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.
Molecular Weight

660.09

Formula

C34H29ClF3N7O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

sEH/AChE-IN-5 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

sEH/AChE-IN-5Cholinesterase (ChE)Epoxide HydrolaseTNF ReceptorInterleukin RelatedTumor Necrosis Factor ReceptorTNFRILSH-SY5YacetylcholinesteraseAlzheimer's diseaseBV-2SMMC7721PC12HepG2ICR miceKunming micesoluble epoxide hydrolaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
sEH/AChE-IN-5
Cat. No.:
HY-183341
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.