GPi688
GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively. GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia.
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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: 918902-32-6
- 分子式: C19H18ClN3O4S
- 分子量:419.88
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
IC50: 19 nM (human liver GPa), 61 nM (rat liver GPa), 12 nM (human skeletal muscle GPa)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
1.1 μM
Compound: 33
|
Inhibition of glucose output in glucagon challenged primary rat hepatocytes
Inhibition of glucose output in glucagon challenged primary rat hepatocytes
|
[PMID: 17095214] |
化学情報
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CAS 番号 918902-32-6
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分子量 419.88
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分子式 C19H18ClN3O4S
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SMILES
O=C(C1=CC(C=C(Cl)S2)=C2N1)NC3C(N(C[C@@H](O)CO)C4=C(C=CC=C4)C3)=O
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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]. Freeman S, et al. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br J Pharmacol. 2006;149(6):775-785. [Content Brief]
[2]. Poucher SM, et al. An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br J Pharmacol. 2007;152(8):1239-1247. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)