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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- CAS No.: 1501974-69-1
- Formule: C21H32FNO7
- Masse moléculaire:429.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
mGluR2 |
mGluR3 |
Chemical Information
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CAS No. 1501974-69-1
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Masse moléculaire 429.48
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)