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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 655237-16-4
- 分子式: C23H24O6
- 分子量:396.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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 |
化学情報
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CAS 番号 655237-16-4
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分子量 396.43
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
YM543 free base 関連分類
HY-122613 関連分類
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