Home Neuronal Signaling GluR agonist VU 0361737

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VU 0361737 GluR agonist

Cat.No.S2892

VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.
VU 0361737 GluR agonist Chemical Structure

Chemical Structure

Molecular Weight: 262.69

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Quality Control

Batch: S289201 DMSO]53 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 100%
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100

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (201.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 262.69 Formula

C13H11ClN2O2

 Storage (From the date of receipt)
CAS No. 1161205-04-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl

Mechanism of Action

Targets/IC50/Ki
mGluR4 (Rat )
110 nM(EC50)
mGluR4 (Human)
240 nM(EC50)
In vitro
VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors.
In vivo
VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1).
References

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