MGS0274
MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.
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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: 1501974-69-1
- 分子式: C21H32FNO7
- 分子量:429.48
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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
製品説明
IC50 & Target
[1]|
mGluR2 |
mGluR3 |
化学情報
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CAS 番号 1501974-69-1
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分子量 429.48
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分子式 C21H32FNO7
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SMILES
O=C([C@@]1(N)[C@]2([H])[C@@H](C(O[C@@H](OC(O[C@H]3[C@H](C(C)C)CC[C@@H](C)C3)=O)C)=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.
プロトコル
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
純度とドキュメンテーション
参考文献
[1]. Urabe H, et al. Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability [published online ahead of print, 2020 Jul 5]. Eur J Med Chem. 2020;203:112521. [Content Brief]
[2]. Kinoshita K, et al. Preclinical disposition of MGS0274 besylate, a prodrug of a potent group II metabotropic glutamate receptor agonist MGS0008 for the treatment of schizophrenia. Pharmacol Res Perspect. 2019;7(5):e00520. Published 2019 Sep 13. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)