Human SGLT2 versus SGLT1 transport inhibition
Cell-based study · Human SGLT2 expressed in 293.ETN cells; human SGLT1 expressed in COS-7 cells. [1]
Radiolabeled AMG uptake showed concentration-dependent inhibition in 25% human plasma. Sodium-free buffer provided the sodium-dependence comparison. Table 1 reports means ± SEM from three independent experiments.
| Endpoint | Reported result | Reference |
|---|---|---|
| Human SGLT2-mediated AMG uptake inhibition | IC50 0.002 ± 0.001 µM | [1] |
| Human SGLT1-mediated AMG uptake inhibition | IC50 5.6 ± 0.59 µM | [1] |
| Reported selectivity for SGLT2 over SGLT1 | Selectivity ratio 2435 | [1] |
Literature-Reported Treatment Conditions
- Exposure duration
- 2 h for SGLT1; 1.5 h for SGLT2
- Method
- Cell-based radiolabeled methyl-α-D-glucopyranoside uptake; scintillation counting at 37 °C.
- Reported limits
- Compound solvent and concentration series are not specified in the inspected assay description/Table 1. IC50 values below are assay endpoints, not treatment doses.
Methods and source locations
Compound reported in the paper: EGT1442; Compound label in the paper: EGT1442, Table 1
Reported EGT1442 material synthesized by Egret Pharma; applicability does not establish Adooq lot identity or potency.
pp. 285–287, §§2.1, 2.3, 2.8, 3.1 and Table 1 (EGT1442 row and footnote)
Human SGLT2-mediated AMG uptake inhibition: Table 1; IC50: mean ± SEM, three independent AMG uptake experiments. Variable-slope nonlinear regression (§2.8). Ratio reported as printed. — p. 287, Table 1, EGT1442 row and footnote; §2.8
Human SGLT1-mediated AMG uptake inhibition: Table 1; IC50: mean ± SEM, three independent AMG uptake experiments. Variable-slope nonlinear regression (§2.8). Ratio reported as printed. — p. 287, Table 1, EGT1442 row and footnote; §2.8
Reported selectivity for SGLT2 over SGLT1: Table 1; IC50: mean ± SEM, three independent AMG uptake experiments. Variable-slope nonlinear regression (§2.8). Ratio reported as printed. — p. 287, Table 1, EGT1442 row and footnote; §2.8