Fatty Acid Amide Hydrolase Human Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
The pharmacological effects of anandamide on CB1 and CB2 receptors depend on the life span of the lipid in the extracellular space, which is limited by a rapid and selective process of cellular uptake, followed by intracellular degradation of anandamide to ethanolamine and arachidonic acid by the enzyme fatty-acid amide hydrolase (FAAH). Representative fatty acid amides degraded by FAAH include the endocannabinoid anandamide and the sleep-inducing lipid oleamide. FAAH may serve as an attractive target for pharmaceutical efforts aimed at influencing endogenous pain and/or sleep-wake systems.
Family:
Lipid Metabolism
Sub Family:
Endocannabinoid Turnover
Protein Name:
Fatty Acid Amide Hydrolase
Uniprot Number:
O00519
Gene Name:
FAAH
Gene ID:
2166
Gene Aliases:
FAAH-1
Accession Number:
NM_001441
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant FAAH expressed in SF21 cells is used. Test compound and/or vehicle are preincubated with 2.6 U/ml‡ of enzyme for 15 minutes at 37⁰C in Tris buffer pH 9.0. The reaction is initiated by addition of 20 µM AMC-AA for another 60 minute incubation period. Read plate on a spectrophotometer (Excitation: 340 nm, Emission: 460 nm). Compounds are screened at 10 μM.
Substrate:
20 µM AMC arachidonoyl amide
Incubation:
60 min at 37°C
Control Inhibitor:
546141-08-6
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:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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