Sotagliflozin (LX4211) | SGLT Inhibitor | CAS 1018899-04-1

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Quality Control

Batch: Purity: 99.67%

99.67

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other SGLT Inhibitors	Phlorizin Phloretin (RJC 02792) Tofogliflozin(CSG 452) Ipragliflozin L-Proline Ipragliflozin (ASP1941) Swertisin KGA-2727 Mizagliflozin (KWA 0711) Bexagliflozin (EGT1442)

Solubility

In vitro
Batch:

DMSO : 250 mg/mL (588.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (4.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

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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.)

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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.

Chemical Information, Storage & Stability

Molecular Weight	424.94	Formula	C₂₁H₂₅ClO₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1018899-04-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LP-802034, LX4211			Smiles	CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)SC)O)O)O)Cl

Mechanism of Action

Targets/IC₅₀/Ki	SGLT2 1.8 nM SGLT1 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.
Kinase Assay	In vitro Human SGLT2/SGLT1 Inhibition Assay
Kinase 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 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22739142/ [2] https://pubmed.ncbi.nlm.nih.gov/23487174/ [3] https://pubmed.ncbi.nlm.nih.gov/25759591/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Sotagliflozin (LX4211) SGLT inhibitor

Chemical Structure

Molecular Weight: 424.94