OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) belongs to the family of oxidoreductases, also known as cortisone reductase, is an NADPH-dependent enzyme that catalyzes conversion of cortisone to cortisol, highly expressed in metabolic tissues including liver, adipose tissue. Over-expression of 11β-HSD1 has been associated with obesity, insulin resistance. 11β-HSD1 inhibition may be useful for treatment of obesity and metabolic syndrome.
Family:
Oxidoreductase
Sub Family:
Oxidase
Class:
Lipid metabolism
Protein Name:
11-beta-HSD1
Uniprot Number:
X5D2L1
Protein Aliases:
11-beta-Hydroxysteroid Dehydrogenase 1
Gene Name:
HSD11B1HSD11B1
Gene ID:
3290
Gene Aliases:
SDR26C1
Accession Number:
NM_181755
Organism:
Human
Construct Details:
Full length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Platform:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant 11-beta-HSD 1 enzyme expressed in HEK293T cells is used. Test compound and/or vehicle is preincubated with 8 µg/ml active enzymeǂ in modified Phosphate buffer pH 7.6 for 15 minutes at 37°C. The reaction is initiated by addition of 1 µM cortisone substrate for another 30 minute incubation period. Determination of the amount of cortisol formed is detected spectrofluorimetrically by Cortisol HTRF kit. Compounds are screened at 10 µM.
Substrate:
1 µM Cortisone
Incubation:
30 min at 37°C
Control Inhibitor:
PF 915275
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uMSuggested concentration for initial testing is 10 uM
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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