R214127
CAS No. : 409345-76-2
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| Cat. No. : | HY-114891 |
| M.Wt: | 303.35 |
| Formula: | C20H17NO2 |
| Purity: | >98 % |
| Solubility: |
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[1].
In Vitro: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].
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