In vitro: LX4211 inhibits [14C]AMG uptake with IC50 of 62.0 nM for mouse SGLT1 and 0.6 nM for mouse SGLT2, respectively. 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 models||Male albino C57BL/6-Tyrc-Brd mice|
|Formulation||Aqueous 0.1% v/v Tween 80|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||84 mg/mL in DMSO|
Sotagliflozin improves glycemic control in nonobese diabetes-prone mice with type 1 diabetes.
Powell DR, et al. Diabetes Metab Syndr Obes. 2015 Feb 26;8:121-7. PMID: 25759591.
LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose.
Powell DR, et al. J Pharmacol Exp Ther. 2013 May;345(2):250-9. PMID: 23487174.
|Related SGLT Products|
Canagliflozin hemihydrate (JNJ-28431754; TA 7284) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM.
|Dapagliflozin ((2S)-1,2-propanediol, hydrate)
Dapagliflozin(BMS512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2) is in development for the treatment of type 2 diabetes mellitus (T2DM).
Phloretin is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes.
Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6.
Canagliflozin is a potent, selective sodium glucose co-transporter 2 inhibitor.
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