R214127
R214127 is a selective mGlu1 receptor antagonist with IC50 values of 6 and 14 nM for rat and human mGlu1a. R214127 acts on a site from the glutamate binding pocket, and competes for the same transmembrane segment VII as other noncompetitive mGlu1 antagonists.
For research use only. We do not sell to patients.
- CAS No.: 409345-76-2
- Formula: C20H17NO2
- Molecular Weight:303.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Rat mGluR1a 6 nM (IC50) |
Human mGluR1a 14 nM (IC50) |
R214127 (Compound 72c) potently inhibits rat mGlu1a receptor signaling in CHO-dhfr cells with an IC50 of 6 nM[1].
R214127 inhibits human mGlu1a receptor signaling in L929sA cells with an IC50 of 14 nM[1].
R214127 (30 μM; 30 min) shows extremely high in vitro metabolism in human liver microsomes, with 99% of the parent compound metabolized[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. 409345-76-2
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Molecular Weight 303.35
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Formula C20H17NO2
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SMILES
O=C(CC1=CC=CC=C1)C2=CC3=CC4=C(OCCC4)N=C3C=C2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)