Methoxymethyl-MTEP
Methoxymethyl-MTEP is a selective, high-affinity mGluR5 antagonist. Methoxymethyl-MTEP can serve as a radiotracer ligand, readily entering the brain and providing mGluR5-specific signal in gray matter regions. Methoxymethyl-MTEP exhibits a Kd = 20 nM as measured by saturation binding assays in rat brain cell membranes, and an IC50 = 30 nM in competitive binding assays. Methoxymethyl-MTEP can be used for research on diseases related to the glutamatergic nervous system, such as excitotoxicity and schizophrenia.
For research use only. We do not sell to patients.
- CAS No.: 524924-75-2
- Formula: C13H12N2OS
- Molecular Weight:244.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
mGluR5 |
In Vitro
Methoxymethyl-MTEP (10 μM) shows negligible binding to a large number of neurotransmitter receptors[1].
The radioactive form of Methoxymethyl-MTEP, [3H]-methoxymethyl-MTEP, can be used for mGlu5 receptor binding and characterization studies[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Methoxymethyl‑MTEP (radioligand; 50 μCi/kg; intravenous injection) exhibits only background levels of specific binding in the forebrain of mGlu5 knockout mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 524924-75-2
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Molecular Weight 244.31
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Formula C13H12N2OS
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SMILES
COCC1=CC(C#CC2=CSC(C)=N2)=CN=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Methoxymethyl-MTEP
- 524924-75-2
- mGluR
- Drug Intermediate
- mGluR5
- glutamate-mediated calcium mobilization
- noncompetitive antagonist
- seven transmembrane domain
- negative allosteric modulator
- NMDA-evoked peak and steady-state currents
- phosphoinositide hydrolysis
- schizophrenia
- excitotoxicity
- MPEP site
- Inhibitor
- inhibitor
- inhibit