Home GPCR & G Protein SGLT inhibitor Sotagliflozin For research use only.

Sotagliflozin

Synonyms: LP-802034, LX4211

Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.

Sotagliflozin Chemical Structure

Sotagliflozin Chemical Structure

CAS No. 1018899-04-1

Purity & Quality Control

Sotagliflozin Related Products

Signaling Pathway

SGLT Signaling Pathways

SGLT Signaling Pathway

Biological Activity

Description Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
Targets
SGLT2 [1] SGLT1 [1]
1.8 nM 36 nM
In vitro
In vitro

LX4211 inhibits [14C]AMG uptake with IC50 of 62.0 nM for mouse SGLT1 and 0.6 nM for mouse SGLT2, respectively. [2]
Kinase Assay In vitro Human SGLT2/SGLT1 Inhibition Assay
Human SGLT2 is cloned into pIRESpuro2 vector for mammalian expression (construct: HA-SGLT2-pIRESpuro2). HEK293 cells are transfected with the human HA-SGLT2-pIRESpuro2 vector and the stably transfected cell line is established in the presence of 0.5 μg/mL of puromycin. Human HA-SGLT2 cells are maintained in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin. The HEK293 cells expressing the human HA-SGLT2 are seeded in 384 well plates (30,000 cells/well) in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin, then incubated overnight at 37 C, 5% CO2. Cells are then washed with uptake buffer (140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 10 mM HEPES, 5 mM Tris, 1 mg/mL bovine serum albumin (BSA), pH 7.3). Twenty microliters of uptake buffer with or without testing compounds are added to the cells. Then, 20 microliters of uptake buffer containing 14C-AMG (100 nCi) are added to the cells. The cell plates are incubated at 37°C, 5% CO2 for 1-2 hours. After washing the cells with uptake buffer, scintillation fluid is added (40 microliters/well) and 14C-AMG uptake is measured by counting radioactivity using a scintillation coulter. Human SGLT1 is cloned into pIRESpuro2 vector for mammalian expression (construct: HA-SGLT1-pIRESpuro2 ). HEK293 cells are transfected with the human HA-SGLT1-pIRESpuro2 vector and the stably transfected cell line is established in the presence of 0.5 μg/mL of puromycin. Human HA-SGLT1 cells are maintained in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin. The HEK293 cells expressing the human HA-SGLT1 were seeded in 384 well plates (30,000 cells/well) in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin, then incubated overnight at 37 C, 5% CO2. Cells were then washed with uptake buffer (140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 10 mM HEPES, 5 mM Tris, 1 mg/mL bovine serum albumin (BSA), pH 7.3). Twenty microliters of uptake buffer with or without testing compounds are added to the cells. Then, 20 microliters of uptake buffer containing 14C-AMG (100 nCi) are also added to cells. The cell plates are incubated at 37°C, 5% CO2 for 1-2 hours. After washing the cells with uptake buffer, scintillation fluid is added (40 microliters/well) and 14C-AMG uptake was measured by counting radioactivity using a scintillation
In Vivo
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. [2]

In nonobese diabetes-prone mice with type 1 diabetes, Sotagliflozin (30 mg/kg) significantly improves glycemic control, without increasing the rate of hypoglycemia measurements. [3]
Animal Research Animal Models Male albino C57BL/6-Tyrc-Brd mice
Dosages ~60 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06147232 Not yet recruiting
Nephropathy|Diabetic Nephropathies|Diabetes Mellitus Type 1|Albuminuria|Diabetic Complications Renal|Diabetic Complications Cardiovascular|Hypoxia
Steno Diabetes Center Copenhagen|Juvenile Diabetes Research Foundation|King''s College London|Glostrup University Hospital Copenhagen
 August 2024 Phase 4
NCT03242018 Completed
Type 2 Diabetes Mellitus|Chronic Kidney Disease Stage 4
Lexicon Pharmaceuticals|Sanofi
 August 16 2017 Phase 3
NCT03174548 Completed
Diabetes Mellitus
Sanofi
 June 12 2017 Phase 1
NCT03070678 Completed
Diabetes Mellitus
Sanofi
 March 14 2017 Phase 1
NCT02926937 Completed
Type 2 Diabetes Mellitus
Lexicon Pharmaceuticals|Sanofi
 November 11 2016 Phase 3

Chemical Information & Solubility

Molecular Weight 424.94 Formula

C21H25ClO5S
CAS No. 1018899-04-1 SDF Download Sotagliflozin SDF
Smiles CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)SC)O)O)O)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (197.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble


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In vivo
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