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.
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- CAS No.: 655237-16-4
- 화학식: C23H24O6
- 분자량:396.43
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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SGLT2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
8.9 nM
Compound: 8e, YM543
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Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-methyl-alpha-D-glucopyranoside accumulation
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-methyl-alpha-D-glucopyranoside accumulation
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[PMID: 23651509] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KK/Ay 2 diabetic mice[1]
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Dosage:0.1, 0.3, 1, and 3 mg/kg
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Administration:oral administration
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Result:Had a strong and sustained antihyperglycemic effect in both KK/Ay type 2 diabetic mice.
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Animal Model:Male Sprague–Dawley rats[1]
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Dosage:1.0 and 3.0 mg/kg
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Administration:intravenous injection (1.0 mg/kg) and oral administration (3.0 mg/kg)
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 655237-16-4
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분자량 396.43
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화학식 C23H24O6
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YM543 free base Related Classifications
HY-122613 Related Classifications
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