[CAS NO. 655237-16-4] YM543 free base
PRODUCTS SPECIFICATIONS [655237-16-4]
DESCRIPTION [655237-16-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 396.43 |
| Molecular Formula | C23H24O6 |
| SMILES | O[C@H]([C@H]1O)[C@@](C2=CC(CC3=CC4=CC=CC=CC4=C3)=CC=C2O)([H])O[C@@H]([C@H]1O)CO |
Summary
IC50 & Target
|
SGLT2 |
In Vivo
YM543 free base (0-3 mg/kg; p.o.) reduces blood glucose levels and improved glucose tolerance with a concomitant increase in urinary glucose excretion in KK/A y 2 diabetic mice, effects that were sustained even after 12 h [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | KK/A y 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: |
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Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [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.