Sotagliflozin (LX4211)

Catalog No.S8103

Sotagliflozin (LX4211) Chemical Structure

Molecular Weight(MW): 424.94

Sotagliflozin (LX4211) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.

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Biological Activity

Description Sotagliflozin (LX4211) 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

LX4211 inhibits [14C]AMG uptake with IC50 of 62.0 nM for mouse SGLT1 and 0.6 nM for mouse SGLT2, respectively. [2]

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]

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: Male albino C57BL/6-Tyrc-Brd mice
  • Formulation: Aqueous 0.1% v/v Tween 80
  • Dosages: ~60 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (197.67 mM)
Ethanol 17 mg/mL warmed (40.0 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 424.94
Formula

C21H25ClO5S

CAS No. 1018899-04-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03174548 Completed Drug: Sotagliflozin (SAR439954) Diabetes Mellitus Sanofi June 12 2017 Phase 1
NCT03070678 Completed Drug: Sotagliflozin (SAR439954)|Drug: Mefenamic acid Diabetes Mellitus Sanofi March 14 2017 Phase 1
NCT02926937 Completed Drug: Sotagliflozin (SAR439954)|Drug: Placebo Type 2 Diabetes Mellitus Sanofi November 11 2016 Phase 3
NCT02384941 Completed Drug: Sotagliflozin|Drug: Placebo Type 1 Diabetes Mellitus Sanofi|Lexicon Pharmaceuticals March 2015 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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SGLT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID