Acetylcholinesterase Human Enzymatic LeadHunter Assay - TW

Item: 104010

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OVERVIEW

DOCUMENTS/REFERENCES

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:

Neurotransmitter Metabolism

Sub Family:

Acetylcholine Turnover

Protein Name:

Acetylcholinesterase

Uniprot Number:

P22303

Protein Aliases:

Yt blood group

Gene Name:

ACHE

Gene ID:

Accession Number:

NM_015831

Organism:

Human

Construct Details:

Fragment, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrophotometry

Measured Response:

Absorbance

Testing Information

Procedure Summary:

Human recombinant acetylcholinesterase expressed in HEK-293 cells is used. Test compound and/or vehicle is preincubated with 4.1 ng/ml of enzyme for 15 minutes at 25oC in phosphate buffer pH 7.4. The reaction is initiated by addition of 0.7 mM acetylthiocholine iodide for another 20-minute incubation period. The product thiocholine reacts with dithiobisnitrobenzoic acid to produce 5-thio-2-nitro-benzoic acid. Determination of the amount of 5-thio-2-nitro-benzoic acid formed is read spectrophotometrically at 405 nm. Compounds are screened at 10 µM.

Substrate:

700 µM Acetylthiocholine

Incubation:

20 min at 25°C

Control Inhibitor:

Physostigmine hydrobromide

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

70137832

Name

Physostigmine hydrobromide

Measurement

0.12μM -

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei