SGLT1 Human Sodium Glucose Cotransporter Functional Cell Based Antagonist Uptake LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
SGLT (sodium-dependent glucose cotransporters) are a family of glucose transporters. The two most well-known members of the SGLT family are SGLT1 and SGLT2. SGLT1 (coded by SLC5A1) is mainly expressed on the apical membrane of the small intestine, kidneys, and heart. As a therapeutic agent, a selective SGLT1 inhibitor may block glucose absorption to treat type 2 diabetes.
Family:
Transporter
Class:
SLC
Protein Name:
Sodium/glucose cotransporter 1
Uniprot Number:
P13866
Protein Aliases:
High affinity sodium-glucose cotransporter, Solute carrier family 5 member 1
Gene Name:
SLC5A1
Gene ID:
6523
Gene Aliases:
D22S675, NAGT, SGLT1
Accession Number:
NM_000343.3
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
High-content Imaging
Platform:
HCA
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human Sodium-Glucose Cotransporter (hSGLT1) expressed in CHO-K1 cells are plated. Test compound and/or vehicle is preincubated with cells (2 x 10⁴/well) in modified HEPES buffer pH 7.4 for 20 minutes at 37°C, 5% CO₂ and 160 µM 1-NBDG is then added for an additional 120 minutes incubation period. Cells are washed by incubation buffer and imaged on ImageXpress Micro Confocal high-content imaging system to determine 1-NBDG uptake. Reduction of 1-NBDG uptake by 50 percent or more (≥50%) relative to 10 µM Sotagliflozin indicates significant inhibitory activity. Compounds are screened at 10, 1, 0.1, 0.01 and 0.001 µM.
Substrate:
1-NBDG
Incubation:
2 hr at 37°C
Control Inhibitor:
Sotagliflozin
Criteria For Significance:
≥ 50% Inhibition of 1-NBDG uptake relative to sotagliflozin 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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