VU 0361737

Catalog No.S2892

For research use only.

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 Chemical Structure

CAS No. 1161205-04-4

Purity & Quality Control

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Biological Activity

Description 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.
Targets
mGluR4 (Rat ) [1] mGluR4 (Human) [1]
110 nM(EC50) 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. [1]

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). [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Sprague-Dawley rats
  • Dosages: 10 mg/kg
  • Administration: ip

Solubility (25°C)

In vitro

DMSO 53 mg/mL
(201.75 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 262.69
Formula

C13H11ClN2O2

CAS No. 1161205-04-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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