MGS0008
MGS0008 is an orally active and brain-penetrant metabotropic glutamate receptor 2/3 (mGlu2/3) agonist with EC50 values of 29.4 nM and 45.4 nM for mGluR2 and mGluR3, respectively. MGS0008 is promising for research of central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases.
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: 234085-20-2
- 分子式: C8H10FNO4
- 分子量:203.17
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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
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mGluR2 29.4 nM (EC50) |
mGluR3 45.4 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>100000 nM
Compound: (+)7
|
Antagonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid
Antagonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid
|
[PMID: 11123999] |
| CHO | EC50 |
>100000 nM
Compound: (+)7
|
Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid
Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid
|
[PMID: 11123999] |
化学情報
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CAS 番号 234085-20-2
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分子量 203.17
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分子式 C8H10FNO4
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SMILES
O=C([C@@]1(N)[C@]2([H])[C@@H](C(O)=O)[C@]2([H])C[C@@H]1F)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]. Ochi M, et al. Bottom-up physiologically based pharmacokinetic modelling for predicting the human pharmacokinetic profiles of the ester prodrug MGS0274 and its active metabolite MGS0008, a metabotropic glutamate 2/3 receptor agonist. Xenobiotica. 2022 Feb;52(2):119-128. [Content Brief]
[2]. Nakazato A, et al. Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists. J Med Chem. 2000 Dec 14;43(25):4893-909. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)