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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
SGLT2 |
Cellular Effect
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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] |
In Vivo
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
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| 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.
Protocol
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
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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