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Sotagliflozin (LX-4211) is an orally active, first-in-class dual SGLT1/2 inhibitor with IC50s of 36 nM and 1.8 nM, respectively, and is used in studies related to type 1 diabetes and heart failure.
In vitro: Sotagliflozin (LX-4211) inhibits [14C]AMG uptake with IC50 of 62.0 nM for mouse SGLT1 and 0.6 nM for mouse SGLT2, respectively.
In vivo: In mice, LX4211 (60 mg/kg, p.o.) reduces intestinal glucose absorption by inhibiting SGLT1, resulting in net increases in GLP-1 and PYY release and decreases in GIP release and blood glucose excursions. In nonobese diabetes-prone mice with type 1 diabetes, Sotagliflozin (30 mg/kg) significantly improves glycemic control, without increasing the rate of hypoglycemia measurements.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Male albino C57BL/6-Tyrc-Brd mice |
| Formulation | Aqueous 0.1% v/v Tween 80 |
| Dosages | ~60 mg/kg |
| Administration | p.o. |
| Molecular Weight | 424.94 |
| Formula | C21H25ClO5S |
| CAS Number | 1018899-04-1 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related SGLT Products |
|---|
| Dapagliflozin
Dapagliflozin (BMS-512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2). |
| Canagliflozin
Canagliflozin is a potent, selective sodium glucose co-transporter 2 inhibitor. |
| Empagliflozin
Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. |
| Phloridzin
Phloridzin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. |
| Phloretin
Phloretin (NSC 407292; RJC 02792) is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). |
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