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product name Sotagliflozin (LX4211)


Description: Sotagliflozin (also known as LX4211) is an orally bioavailable, dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Sotagliflozin improves glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Sotagliflozin also increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose.           

References: J Pharmacol Exp Ther. 2013 May;345(2):250-9; Diabetes Metab Syndr Obes. 2015 Feb 26;8:121-7.



Molecular Weight (MW)

424.94
Formula

C21H25ClO5S
CAS No.

1018899-04-1
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 84 mg/mL (197.7 mM) 
Water: <1 mg/mL
Ethanol: 17 mg/mL (40.0 mM)
Solubility (In vivo)

 
Synonyms

LX4211

other peoduct :

In Vitro

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


Kinase Assay:  


Cell Assay

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.
Animal model Male albino C57BL/6-Tyrc-Brd mice
Formulation & Dosage Dissolved in aqueous 0.1% v/v Tween 80; 60 mg/kg; oral administration.
References J Pharmacol Exp Ther. 2013 May;345(2):250-9; Diabetes Metab Syndr Obes. 2015 Feb 26;8:121-7.

GDC-0837

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Author: Sodium channel