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Cat. No.: HY-114891

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

R214127 Chemical Structure

CAS No.: 409345-76-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

Rat mGluR1a

6 nM (IC₅₀)

Human mGluR1a

14 nM (IC₅₀)

All mGluR Isoforms :

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. Further protocols information, click here.

Chemical Information

CAS No. 409345-76-2
Molecular Weight 303.35
Formula C₂₀H₁₇NO₂
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.

Protocols

All Cell Biology

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

Handling Instructions (2659 KB)

References

[1]. Mabire D, et al. Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J Med Chem. 2005;48(6):2134-2153. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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