Biological Information

Background Information:

Acetylcholinesterase (ACES, AchE, EC 3.1.1.7)) terminates the action of acetylcholine (ACh) at the junctions of various cholinergic nerve endings with their effector organs or postsynaptic sites. Compounds that inhibit AChE are called anticholinesterase agents and are used to ameliorate the symptoms of myesthenia gravis, lower intraocular pressure in glaucoma and for possible treatment of dementia through increase of ACh concentration in the brain. Anticholinesterases may also cause salivation, meiosis, increase in gastrointestinal motility, skeletal muscle paralysis, respiratory arrest and cardiovascular collapse. These agents are also used as insecticides and pesticides for agricultural purposes and vector control.

Family:

Enzyme

Sub Family:

Acetylcholine turnover

Protein Name:

AChE

Uniprot Number:

P22303

Protein Aliases:

Yt blood group

Gene Name:

ACHE

Gene ID:

43

Accession Number:

NM_015831

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrophotometric

Testing Information

Substrate:

Acetylthiocholine (400 µM)

Incubation:

30 min at RT

Control Inhibitor:

galanthamine

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

1935

Name

Tacrine

Measurement

63nM - IC50

PubChem ID

4456

Name

NEOSTIGMINE

Measurement

31nM - IC50

PubChem ID

9651

Name

galanthamine

Measurement

520nM - IC50

PubChem ID

70137832

Name

Physostigmine hydrobromide

Measurement

20nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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