IBAT Human Ileal Bile Acid Transporter Functional Cell Based Antagonist Uptake LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Ileal bile acid transporter (IBAT), also known as ASBT (apical sodium-bile acid transporter, encoded by SLC10A2), is enriched in intestine and has physiological function in the enterohepatic recirculation of bile acids and cholesterol metabolism. IBAT inhibition may have potential to treat hypercholesterolemia and colonic motor activity.
Family:
Transporter
Class:
SLC
Accession Number:
NM_000452
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human ileal sodium/bile acid cotransporter (IBAT) expressed in HEK-293T/17 cells are plated. Test compound and/or vehicle is preincubated with cells (3 x 10^5/ml) in modified HBSS buffer for 20 minutes at 37C and 150 nM [3H]TCA is then added for an additional 30 minute incubation period. A lysate is obtained from solubilized cells and counted to determine [3H]TCA uptake. Reduction of [3H]TCA uptake by 50 percent or more (≥50%) relative to 10 µM Linerixibat indicates significant inhibitory activity.
Incubation:
30 min at 37°C
Control Inhibitor:
Linerixibat
Criteria For Significance:
≥ 50% Inhibition of [3H]TCA uptake relative to linerixibat response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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