Sotagliflozin (LX4211)

Catalog No.S8103 Synonyms: LP-802034

For research use only.

Sotagliflozin (LX4211, LP-802034) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.

Sotagliflozin (LX4211) Chemical Structure

CAS No. 1018899-04-1

Selleck's Sotagliflozin (LX4211) has been cited by 7 Publications

Purity & Quality Control

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Biological Activity

Description Sotagliflozin (LX4211, LP-802034) 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 (from reference)

Animal Research:[2]
  • Animal Models: Male albino C57BL/6-Tyrc-Brd mice
  • Dosages: ~60 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 424.94
Formula

C21H25ClO5S

CAS No. 1018899-04-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)SC)O)O)O)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03242018 Completed Drug: Placebo|Drug: Sotagliflozin Type 2 Diabetes Mellitus|Chronic Kidney Disease Stage 4 Lexicon Pharmaceuticals|Sanofi August 16 2017 Phase 3
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 Lexicon Pharmaceuticals|Sanofi November 11 2016 Phase 3
NCT01292993 Completed Drug: 400 mg LX4211|Drug: 1000 mg metformin Type 2 Diabetes Mellitus Lexicon Pharmaceuticals February 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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