2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. 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.

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R214127

R214127 Chemical Structure

CAS No. : 409345-76-2

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R214127 Related Antibodies

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Description

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].

IC50 & Target[1]

Rat mGluR1a

6 nM (IC50)

Human mGluR1a

14 nM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

R214127 Related Antibodies
Molecular Weight

303.35

Formula

C20H17NO2
CAS No.
SMILES

O=C(CC1=CC=CC=C1)C2=CC3=CC4=C(OCCC4)N=C3C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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R214127 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R214127409345-76-2R 214127R-214127mGluRMetabotropic glutamate receptorsCHO-dhfr cellshuman mGlu1a receptortransmembrane segment VIIglutamate binding pocketmGlu1 receptorhuman liver microsomesrat mGlu1a receptorL929sA cellsInhibitorinhibitorinhibit

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