YM543 free base

YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes[1][2].

Research Areas >> Metabolic Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> SGLT

SGLT2

YM543 free base (0-3 mg/kg; p.o.) 在 KK/Ay 2 型糖尿病小鼠中降低血糖水平并改善葡萄糖耐量，同时增加尿糖排泄，效果甚至在 12 小时后仍持续[1]。 Animal Model: KK/Ay 2 diabetic mice[1] Dosage: 0.1, 0.3, 1, and 3 mg/kg Administration: oral administration Result: Had a strong and sustained antihyperglycemic effect in both KK/Ay type 2 diabetic mice. Animal Model: Male Sprague–Dawley rats[1] Dosage: 1.0 and 3.0 mg/kg Administration: intravenous injection (1.0 mg/kg) and oral administration (3.0 mg/kg) Result: 1.19 Administration iv (1 mg/kg) po (3 mg/kg) T1/2 (h) 0.9 1.3 CLtot (L/h/kg) 2483 Vdss (L/kg) 3360 Cmax (ng/mL) 101 Tmax (h) 0.5 AUC0-inf (ng h/mL) 403 F % 29

[1]. Ikegai K, et, al. Synthesis and biological evaluation of C-glucosides with azulene rings as selective SGLT2 inhibitors for the treatment of type 2 diabetes mellitus: discovery of YM543. Bioorg Med Chem. 2013 Jul 1;21(13):3934-48.  

[2]. Nakada N. Evaluation of the Utility of Chimeric Mice with Humanized Livers for the Characterization and Profiling of the Metabolites of a Selective Inhibitor (YM543) of the Sodium-Glucose Cotransporter 2. Pharm Res. 2017 Apr;34(4):874-886.